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=> s affective () disorder? 

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=> 11 and rev.i©w/dt 

1873001 REVIEW/DT 
L2 599 LI AND REVIEW/DT 

=> s 12 and autism 

1297 AUTISM 
L3 8 L2 AND AUTISM 

=> d 13, ibib ahs, 1-8 

L3 ANSWER 1 OF 8 HCAPLUS COPYRIGHT 2005 ACS on STN 



ACCESSION NUMBER 
TITLE: 



AUTHOR (S) : 
CORPORATE SOURCE 

SOURCE : 

PUBLISHER: 
DOCUMENT TYPE: 
LANGUAGE : 
AB 



2005:970365 HCAPLUS 

Immunological etiology of major psychiatric disorders: 
evidence and therapeutic implications 
Sperner-Unterweger, Barbara 

Department of Biological Psychiatry, Innsbruck 
University Clinics, Innsbruck, Austria 
Drugs (2005), 65(11), 1493-1520 
CODEN: DRUGAY; ISSN: 0012-6667 
Adis International Ltd. 
Journal; General Review 
English 

A review. Historically, Immunol . research in psychiatry was based on 
empirical findings and early epidemiol . studies indicating a possible 
relation between psychiatric symptoms and acute infectious diseases. 
However, aetiopathol . explanations for psychiatric disorders are no longer 
closely related to acute infection. Nevertheless, immune hypotheses have 
been discussed in schizophrenia, affective disorders and infantile 
autism in the last decades. Although the variability between the 
results of the epidemiol, studies conducted to date is strikingly high, 
there is still some evidence that the immune system might play a role in 
the aetiopathogenesis of these three psychiatric diseases, at least in 
subgroups of patients- In anxiety disorders immunol . research is still 
very much in its infancy, and the few and inconsistent data of immune 
changes in these patients are believed to reflect the influence of short- 
er long-term stress exposure. Nevertheless, there are also some hints 
raising the possibility that autoimmune mechanisms could interrupt 
neurotransmission, which would be of significance in certain patients with 
anxiety, and panic disorders. Drug and ale. (ethanol) dependence are not 
believed to be primarily influenced by an immunol. etiol. Immune 
reactions due to different drugs of abuse and ale. may directly or 
indirectly influence the course of concomitant somatic diseases. In 
different org. brain disorders the underlying somatic disease is defined 
as a primary immune or autoimmune disorders, for example AIDS and SLE . 
Therapeutic approaches in Alzheimer's disease also apply immunol. methods 
such as strategies of active/passive immunization and NSAIDs. Considering 
the comprehensive interactive network between mind and body, future 
research should focus on approaches linking targets of the different 
involved systems, 

REFERENCE COUNT: 408 THERE ARE 408 CITED REFERENCES AVAILABLE FOR 

THIS. RECORD. ALL CITATIONS AVAILABLE IN THE RE 
FORMAT 

^^A^^^t2^ 8 HCAPLUS COPYRIGHT 2005 ACS on STN 
ACCESSION NUMBER: 2004:31945 HCAPLUS 



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DOCUMENT NUMBER: 
TITLE: 

AUTHOR (S): 
CORPORATE SOURCE 



140:197018 

Genetic analysis of psychiatric disorders associated 
with human chromosome 18 
Kamnasaran, Deepak 

The Arthur and Sonia Labatts Brain Tumour Research 
Centre, The Hospital for Sick Children, Toronto, ON, 
Can. 

SOURCE: Clinical and Investigative Medicine (2003), 26(6), 

285-302 

CODEN: CNVMDL; ISSN: 0147-958X 
PUBLISHER: Canadian Medical Association 

DOCUMENT TYPE: Journal; General Review 

LANGUAGE: English 

AB A review. Current models on the etiol. of psychiatric disorders support 
the idea of a biol. cause as well as interactions of biol. systems with 
the environment. The elucidation of the genetic etiol. is of paramount 
importance to understand the cause of psychiatric disorders. Human 
chromosome 18 was identified as one of the first chromosomes to be 
aberrant in psychiatric patients and has subsequently served as a model to 
identify the mol. cause. In this article I review a multitude of 
methodologies that can be used in detg. the genetic basis of 
schizophrenia, affective disorder and autism assocd. with human 
chromosome 18. These strategies include the use of chromosome 
aberrations, linkage and assocn. studies, mouse-human comparative 
genomics, mutation anal, on candidate genes, trinucleotide repeat 
expansion studies, search for genes demonstrating parental effects and 
bioinformatics. Current data from the use of these methods are cited from 
the literature. Linkage and assocn. studies have suggested at least 2 
candidate loci on the short and long arms of chromosome 18 for each of 
these psychiatric disorders. Some loci are supported by the mapping of 
chromosome aberrations from psychiatric patients. Mutation analyses of 
psychiatric patients with 4 candidate genes (NEDD4L, IMPA2, PACAP and 
GNAL) mapping within these loci have been unsuccessful, although an 
assocn. was found with the IMPA2 gene in patients " with schizophrenia. 
With these methods and findings, our understanding of the cause of 
psychiatric disorders assocd. with human chromosome 18 has improved and 
will advance, esp. with emerging data from the human and rodent genome 
projects . 

REFERENCE COUNT: 60 THERE ARE 60 CITED REFERENCES AVAILABLE FOR THIS 

RECORD. ALL CITATIONS AVAILABLE IN THE RE FORMAT 



ANSWER 3 OF 8 HCAPLUS COPYRIGHT 2005 ACS on STN 




ACCESSION NUMBER: 
DOCUMENT NUMBER: 
TITLE : 

AUTHOR (S) : 
CORPORATE SOURCE: 

SOURCE : 



DOCUMENT TYPE: 



2001: 675801 HCAPLUS 
136:67782 

Serotonin transporter: From genomics and knockouts to 
behavioral traits and psychiatric disorders 
Lesch, Klaus-Peter 

Department of Psychiatry and Psychotherapy, University 
of Wurzburg, Wurzburg, Germany 

Molecular Genetics of Mental Disorders: The Place of 
Molecular Genetics in Basic Mechanisms and Clinical 
Applications in Mental Disorders, [Papers presented at 
an International Symposium], Castres, France, Dec. 
1-3, 1999 (2001), Meeting Date 1999, 221-267. 
Editor(s): Briley, Mike; Sulser, Fridolin. Martin 
Dunitz Ltd. : London,, UK. 
CODEN: 69BUOE 

Conference; General Review 



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LANGUAGE: English 

AB A review discusses the possible role of serotonin transporter gene in the 
integration of synaptic connections in the mammalian brain during 
development, adult life, and old age. Allelic variation in functional 
5-HTT expression may play a crit. role in synaptic plasticity, thus 
setting the stage for expression of complex traits and their assocd. 
behavior throughout adult life. Genetically driven variation of 5-HTT 
function, in conjunction with other predisposing genetic factors and with 
inadequate adaptive responses to environmental stressors, is also likely 
to contribute to the etiopathogenesis and treatment response of affective 
spectrum disorders emerging from compromised brain development and from 
neuroadaptive processes. 

REFERENCE COUNT: 173 THERE ARE 173 CITED REFERENCES AVAILABLE FOR 

THIS RECORD. ALL CITATIONS AVAIL7\BLE IN THE RE 
FORMAT 



L3 ANSWER 4 OF 8 HCAPLUS COPYRIGHT 2005 ACS on STN 



HCAPLUS 



Full s 
Text metmsn^es 



ACCESSION NUMBER 
DOCUMENT NUMBER: 
TITLE: 



AUTHOR (S) : 
CORPORATE SOURCE 

SOURCE : 



PUBLISHER: 
DOCUMENT TYPE 
LANGUAGE : 
AB 



. 2001:483884 
136: 132313 

The effects of tryptophan depletion on mood and 
psychiatric symptoms 
Van der Does, A. J. W. 

Departments of Psychology and Psychiatry, Leiden 
University, Leiden, 2333 AK, Neth. 
Journal of Affective Disorders (2001), 64(2-3), 
107-119 

■ CODEN: JADID7; ISSN: 0165-0327 
Elsevier Science B.V. 
Journal; General Review 
English 

A review. The no. of studies using Trp depletion (TD) challenge has 
increased markedly in the past few years. Recently, a no. of neg. results 
were published, implicating that the effect of TD on mood may be less 
consistent than previously thought. The literature on the mood effects of 
TD in psychiatric patients and healthy volunteers was reviewed. TD has a 
mood-lowering effect in subgroups of recovered depressed patients, 
patients with seasonal affective disorder and vulnerable healthy 
subjects. The mood effect in former patients is of a different quality, 
however, than the effect in healthy subjects. Some recent neg. studies in 
depression might be explained by insufficient lowering of plasma Trp 
levels. Preliminary evidence exists for an effect of TD on bulimia 
nervosa, autism, aggression and substance dependence. Conclusions: The 
effects of TD on mood may be more consistent than suggested by a no. of 
recent neg. studies. Response to TD in recovered depressed patients is 
assocd. with prior treatment. However, even in SSRI-treated patients the 
relapse rates are not higher than 50-60%, which needs to be explained. 
The Clin, usefulness of the response to TD in recovered patients 
(prediction of relapse after treatment discontinuation) and in symptomatic 
patients (prediction of treatment refractoriness) deserves more research 
attention. Further suggestions for future research include the cognitive 
effects of TD in recovered depressed patients and the effect of dietary 
habits on response to TD. 
REFERENCE COUNT: 82 THERE ARE 82 CITED REFERENCES AVAILABLE FOR THIS 

RECORD. ALL CITATIONS AVAILABLE IN THE RE FORMAT 



L3 ANSWER 5 OF 8 HCAPLUS COPYRIGHT 2005 ACS on STN 




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ACCESSION NUMBER 
DOCUMENT NUMBER: 
TITLE : 



AUTHOR (S) : 



CORPORATE SOURCE: 



SOURCE : 



2000: 672769 HCAPLUS 
134:264009 

Soma disease virus infection of adult and neonatal 
rats: models for neuropsychiatric disease 
Hornig, Mady; Weissenbock, Herbert; Horscroft, Nigel; 
O'Rourke, Lisa M.; Lipkin, W. Ian 

Emerging Diseases Laboratory, Department of Neurology, 
College of Medicine, University of California, Irvine, 
USA 

Advances in Animal Virology, Papers presented at the 
ICGEB-UCI Virology Symposium, 2nd, New Delhi, India, 
Nov. 9-11, 1998 (2000), Meeting Date 1998, 171-186. 
Editor(s): Jameel, Shahid; Villarreal, Luis P. 
Science Publishers, Inc.: Enfield, N. H. 
CODEN: 69AKWL 
Conference; General Review 
English 

A review with 76 refs. regarding the establishment of a new animal model 
for disorders of monoamine circuitry such as autism, schizophrenia, and 
affective disorders based on persistent viral infection. This model 
demonstrates that the manifestations of infection are dependent upon 
complex interactions between the infectious agent and the host. Crit. 
features in detg. the nature of disease are the status of the immune 
system, and the relative maturity of the central nervous system. 
REFERENCE COUNT: 76 THERE ARE 7 6 CITED REFERENCES AVAILABLE FOR THIS 

RECORD. ALL CITATIONS AVAILABLE IN THE RE FORMAT 



DOCUMENT TYPE 
LANGUAGE : 
AB 



L3 



ANSWER 6 OF 8 HCAPLUS COPYRIGHT 2005 ACS on STN 



HCAPLUS 



ACCESSION NUMBER: 
DOCUMENT NUMBER: 
TITLE: 
AUTHOR (S) : 
CORPORATE SOURCE: 



SOURCE : 

PUBLISHER: 
DOCUMENT TYPE 
L7\NGUAGE : 
AB 



1999:675206 
132:145966 

Psychopharmacology in autism 
Tsai, Luke Y. 

University of Michigan Medical School and 
Developmental Disorders Clinic, University of Michigan 
Medical Center, Child and Adolescent Psychiatric 
Hospital, Ann Arbor, MI, 48109-0390, USA 
Psychosomatic Medicine (1999), 61(5), 651-665 
CODEN: PSMEAP; ISSN: 0033-3174 
Lippincott Williams & Wilkins 
Journal; General Review 
English 

A review with 122 refs. Autism is a neurobiol. disorder. The core 
clin. features of autism include impairment in social interaction, 
impairments in verbal and nonverbal communication, and restricte,d, 
repetitive, and stereotyped patterns of behavior, interests, and 
activities. Autism often has coexisting neuropsychiatric disorders, 
including seizure disorders, attention deficit hyperactivity disorder, 
affective disorders, anxiety disorder, obsessive-compulsive disorder, 
and Tourette disorder. No etiol . -based treatment modality has been 
developed to cure individuals with autism. However, comprehensive 
intervention, including parental counseling, behavior modification, 
special education in a highly structured environment, sensory integration 
training, speech therapy, social skill training, and medication, has 
demonstrated significant treatment effects in many individuals with 
autism. Findings from preliminary studies of major neurotransmitters 
and other neurochem. agents strongly suggest that neurochem. factors play 
a major role in autism. The findings also provide the rationale for 
psychopharmacotherapy in individuals with autism. This article reviews 



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studies of neurochem. systems and related psychopharmacol , research in 
autism and related neuropsychiatric disorders. Clin, indications for 
pharmacotherapy are described, and uses of various medications are 
suggested. This article also discusses new avenues of investigation that 
may lead to the development of more effective medication treatments in 
persons with autism. 
REFERENCE COUNT: 122 THERE ARE 122 CITED REFERENCES AVAILABLE FOR 

THIS RECORD. ALL CITATIONS AVAILABLE IN THE RE 

FORMAT 



ANSWER 7 OF 8 




ACCESSION NUMBER 
DOCUMENT NUMBER: 
TITLE: 



HCAPLUS COPYRIGHT 2005 ACS on STN 



HCAPLUS 



AUTHOR (S) : 
CORPORATE SOURCE: 
SOURCE : 

DOCUMENT TYPE: 
LANGUAGE : 
AB 



1993:557120 
119:157120 

Genes with triplet repeats: candidate mediators of 

neuropsychiatric disorders 

Ross, Christopher A.; Mclnnis, Melvin G.; Margolis, 
Russell L.; Li, Shi Hua 

Sch. Med., Johns Hopkins Univ., Baltimore, MD, 
21205-2196, USA 

Trends in Neurosciences (1993), 16(7), 254-60 
CODEN: TNSCDR; ISSN: 0166-2236 
Journal; General Review 

English 

A review with 90 refs. on the diseases of fragile X syndrome, spinal and 
bulbar muscle atrophy, myotonic dystrophy and the diseases of fragile 
Huntington's disease. Three are characterized by unusual patterns of 
inheritance, in particular, genetic anticipation in which the severity of 
the disorder increases and the age of onset decreases in successive 
generations of a pedigree. Several idiopathic neuropsychiatric disorders 
have features of inheritance consistent with anticipation. In bipolar 
affective disorder, there is evidence for both earlier age of onset 
and more severe illness in the second generation of a subset of unilineal 
pedigrees. There is also the suggestion of anticipation in some forms of 
schizophrenia, spinocerebellar atrophy and autism. Triplet repeats are 
present in addnl . known genes, both in coding regions and untranslated 
regions. Furthermore, many novel genes with triplet repeats are expressed 
in the human brain, and these are candidates to cause some forms of these 
neuropsychiatric disorders. 



L3 ANSWER 8 OF 8 HCAPLUS COPYRIGHT 2005 ACS on STN 



ACCESSION NUMBER: 
DOCUMENT NUMBER: 
TITLE: 
AUTHOR (S) : 
CORPORATE SOURCE: 

SOURCE : 



DOCUMENT TYPE: 

LANGUAGE : 

AB A review with 
schizophrenia, 
self-injurious 



1992:56382 HCAPLUS 
116:56382 

The opioid model in psychiatric research 
Frecska, Ede; Davis, Kenneth L. 

Dep. Psychiatry, Mount Sinai Med. Cent., New York, 
USA 

Progress in Psychiatry (1991), 29 (Neuropept . 
Psychiatr. Disord.), 169-91 
CODEN: PPSHED; ISSN: 1070-1443 
Journal; General Review 

English 

-100 refs. of endogenous opioid peptides role in 
affective disorders, childhood autism and 
behavior, and eating disorders. 



NY, 



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=> s cerebral O function <) disorder? 
91771 CEREBRAL 
1339312 EWCTION 

416929 FUNCTIONS 
1614475 FUNCTION 

(FUNCTION OR FUNCTIONS) 
409471 DISORDER? 
L4 15 CEREBRAL (W) FUNCTION (W) DISORDER? 

=> s 14 and autism? 

1297 AUTISM? 
L5 1 L4 AND AUTISM? 

=> d 15, ibib abs, 1 

L5 ANSWER 1 OF 1 HCAPLUS COPYRIGHT 2005 ACS on STN 



ACCESSION NUMBER: 
DOCUMENT NUMBER: 
TITLE: 

INVENTOR (S) : 

PATENT ASSIGNEE (S) : 
SOURCE : 



DOCUMENT TYPE: 
LANGUAGE : 

FAMILY ACC. NUM. COUNT: 
PATENT INFORMATION: 



2002:72805 HCAPLUS 
136: 139829 

Compositions comprising sibutramine metabolites in 
combination with phosphodiesterase inhibitors 
Jerussi, Thomas P.; Senanayake, Chrisantha H.; Fang, 
Qun K. 

Sepracor, Inc., USA 

U.S. Pat. Appl. Publ., 24 pp., Cont . -in-part of U.S. 

Ser. No. 662,135. 

CODEN: USXXCO 

Patent 

English 

5 



PATENT NO. 



KIND DATE 



APPLICATION NO. 



DATE 



US 


2002010198 




Al 




20020124 




US 2001- 


770663 




20010129 


us 


6476078 






B2 




20021105 
















us 


6331571 






Bl 




20011218 




US 1999- 


372158 




19990811 


EP 


1475086 






A2 




20041110 




EP 2004- 


18454 




19990823 




R: AT, 


BE, 


CH, 


DE, 


DK, 


ES, 


FR, 


GB, 


GR, IT, 


LI, 


LU, 


NL, 


SE, MC, 


PT, 




IE, 


SI, 


LT, 


LV, 


FI, 


RO, 


MK, 


CY, 


AL 












US 


6339106 






Bl 




20020115 




US 2000- 


662135 




20000914 


wo 


2002060424 




A2 




20020808 




WO 2002- 


US2040 




20020123 


wo 


2002060424 




A3 




20030206 


















W: AE, 


AG, 


AL, 


AM, 


AT, 


AU, 


AZ, 


BA, 


BB, BG, 


BR, 


BY, 


BZ, 


CA, CH, 


CN, 




... CO, 


CR, 


CU, 


CZ, 


DE, 


DK, 


DM, 


DZ, 


EC, EE, 


ES, 


FI, 


GB, 


GD, GE, 


GH, 




GM, 


HR, 


HU, 


ID, 


IL, 


IN, 


IS, 


JP, 


KE, KG, 


KP, 


KR, 


KZ, 


LC, LK, 


LR, 




LS, 


LT, 


LU, 


LV, 


MA, 


MD, 


MG, 


MK, 


MN, MW, 


MX, 


MZ, 


NO, 


NZ, OM, 


PH, 




PL, 


PT, 


RO, 


RU, 


SD, 


SE, 


SG, 


SI, 


SK, SL, 


TJ, 


TM, 


TN, 


TR, TT, 


TZ, 




UA, 


UG, 


UZ, 


VN, 


YU, 


2A, 


ZM, 


ZW, 


AM, AZ, 


BY, 


KG, 


KZ, 


MD, RU, 


TJ, TM 




RW: GH, 


GM, 


KE, 


LS, 


MW, 


MZ, 


SD, 


SL, 


SZ, TZ, 


UG, 


ZM, 


ZW, 


AT, BE, 


CH, 




CY, 


DE, 


DK, 


ES, 


FI, 


FR, 


GB, 


GR, 


IE, IT, 


LU, 


MC, 


NL, 


PT, SE, 


TR, 




BF, 


BJ, 


CF, 


CG, 


CI, 


CM, 


GA, 


GN, 


GQ, GW, 


ML, 


MR, 


NE, 


SN, TD, 


TG 


US 


2003096792 




Al 




20030522 




US 2002- 


278097 




20021023 


US 


2003195261 




Al 




20031016 




US 2003- 


395298 




20030325 


us 


2004067957 




Al 




20040408 




US 2003- 


665448 




20030922 


US 


2004092481 




Al 




20040513 




US 2003- 


693980 




20031028 


us 


2004116534 




Al 




20040617 




US 2003- 


717653 




20031121 


us 


2004162355 




Al 




20040819 




US 2004- 


769860 




20040203 


us 


2004180857 




Al 




20040916 




US 2004- 


806415 




20040323 



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PRIORITY APPLN. INFO.: US 1999-372158 A2 19990811 

A2 20000914 
P 19980824 
P 19980902 
A3 19990823 
A3 19991001 
A 20010129 
A3 20011204 
A3 20020604 
A3 20021023 



US 


2000- 


662135 


us 


1998- 


97665P 


us 


1998- 


99306P 


EP 


1999- 


945137 


us 


1999- 


409889 


us 


2001- 


770663 


us 


2001- 


806 


us 


2002- 


160033 


us 


2002- 


278097 



AB Methods are disclosed for the treatment and prevention of disorders and 

conditions such as, but are not limited to: eating disorders; wt. gain; 
obesity; irritable bowel syndrome; obsessive-compulsive disorders; 
platelet adhesion; apnea; affective disorders such as attention deficit 
disorders, depression, and anxiety; male and female sexual function 
disorders; restless leg syndrome; osteoarthritis; substance abuse 
including nicotine and cocaine addiction; narcolepsy; pain such as 
neuropathic pain, diabetic neuropathy, and chronic pain; migraines; 
cerebral function disorders; chronic disorders such as premenstrual 
syndrome; and incontinence. Pharmaceutical compns. and dosage forms are 
also disclosed which comprise a racemic or optically pure sibutramine 
metabolite and an optional drug. Sibutramine free base was prepd. by the 
reaction of chlorbenzylnitrile dibromopropane in the presence of NaH in 
DMSO, followed by the treatment of the resulting l-(4- 

chlorophenyl) cyclobutanecarbonitrile with isobutylmagnesium bromide and 
finally treatment with HCHO. The fee base was resolved into the (R) and 
(S) isomers and converted into their metabolites. Hard gelatin capsules 
contained racemic or optically pure sibutramine metabolite 5.0, 
microcryst. cellulose 90.0, pregelatinized starch 100.3, croscarmellose 
sodium 7.0, and Mg stearate 0.2 mg. 



1158 VENLAFAXINE 

1 VENLAFAXINES 
1158 VENLAFAXINE 

(VENLAFAXINE OR VENLAFAXINES) 
1297 AUTISM? 
L6 1 VENLAFAXINE (W) AUTISM? 

=> s 16 and review /dt 

1873001 REVIEW/DT 
L7 0 L6 AND REVIEW/DT 

=> d 16, ibib csbs, 1 



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2004 : 1064323 HCAPLUS 
142:403954 

Venlafaxine has modest effects in autistic children 
Niederhofer, Helmut 

Reparto di Pediatria, Regional Hospital of Bolzano, 

Bolzano, 39100, Italy 

Therapy (2004), 1(1), 87-90 

CODEN: THERCR 

Future Drugs Ltd. 

Journal 

English 



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AB Objectives: Few controlled psychopharmacol . trials have been conducted in 
autistic children to det. which agents may be effective at alleviating 
assocd, symptoms. Methods: Fourteen male children (7.173.0 years) with 
autistic disorder, diagnosed by ICD-10 criteria, completed a 
placebo-controlled, double-blind crossover trial of venlafaxine (Effexord, 
Wyeth) administered at a dosage of 30 mg daily for 6 wk. Subjects were 
included in the study if their eye contact and expressive language were 
inadequate for their developmental level. Subjects had not tolerated or 
responded to other psychopharmacol. treatments (neuroleptics, 
methylphenidate, clonidine or desipramine) . Results: Teacher ratings on 
the Aberrant Behavior Checklist irritability, stereotype and inappropriate 
speech factors were lower during treatment with venlafaxine than during 
treatment with placebo. Clinician ratings (Children's Psychiatric Rating 
Scale Autism, Anger and Speech Deviance factors; Children's Global 
Assessment Scale; Clin. Global Impressions Efficacy) of videotaped 
sessions were not significantly different between venlafaxine and placebo. 
Discussion: Venlafaxine was modestly effective in the short-term treatment 
of irritability in some children with autistic disorder. 

REFERENCE COUNT: 16 THERE ARE 16 CITED REFERENCES AVAILABLE FOR THIS 

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=> s venlafaxirje () n€iX3rodegen©ratlve {) disorder? 
1158 VENLAFAXINE 

1 VENLAFAXINES 
1158 VENLAFAXINE 

(VENLAFAXINE OR VENLAFAXINES) 
14262 NEURODEGENERATIVE 

1 NEURODEGENERATIVES 
14262 NEURODEGENERATIVE 

(NEURODEGENERATIVE OR NEURODEGENERATIVES) 
409471 DISORDER? 
L8 0 VENLAFAXINE (W) NEURODEGENERATIVE (W) DISORDER? 

=> d his 

(FILE 'HOME* ENTERED AT 18:51:56 ON 22 NOV 2005) 
FILE 'REGISTRY* ENTERED AT 18:52:03 ON 22 NOV 2005 
FILE 'HCAPLUS' ENTERED AT 18:52:06 ON 22 NOV 2005 



LI 2114 S AFFECTIVE () DISORDER? 

L2 599 S LI AND REVIEW/DT 

L3 8 S L2 AND AUTISM 

L4 15 S CEREBRAL () FUNCTION () DISORDER? 

L5 1 S L4 AND AUTISM? 

L6 IS VENLAFAXINE () AUTISM? 

L7 d S L6 AND REVIEW/DT 

L8 OS VENLAFAXINE () NEURODEGENERATIVE {) DISORDER? 



=> s central {) nervoxis () system () disorder? 
361421 CENTRAL 

25 CENTRALS 
361444 CENTRAL 

(CENTRAL OR CENTRALS) 
192233 NERVOUS 
2184797 SYSTEM 
1202882 SYSTEMS 
2965993 SYSTEM 

(SYSTEM OR SYSTEMS) 



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409471 DISORDER? 
L9 814 CENTRAL (W) NERVOUS (W) SYSTEM (W) DISORDER?' 

=> s 19 () autisra? 

1297 AUTISM? 
LIO 0 L9 (W) AUTISM? 

=> s 19 and autism? 

1297 AUTISM? 
Lll 23 L9 AND AUTISM? 

=> s 111 and reviaw/dt 

1873001 REVIEW/DT 
LI 2 1 Lll AND REVIEW/DT 

=> d 112, ib±h ahs, 1 

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ACCESSION NUMBER: 2002:532960 HCAPLUS 

DOCUMENT NUMBER: 138:82774 

TITLE: Aniracetam: its novel therapeutic potential in 

cerebral dysfunctional disorders based on recent 
pharmacological discoveries 

AUTHOR(S): Nakamura, Kazuo 

CORPORATE SOURCE: Clinical PK Laboratory, Department of Product 

Research, Nippon Roche Research Center, Kamakura, 
Japan 

SOURCE: CNS Drug Reviews (2002), 8(1), 70-89 

CODEN: CDREFB; ISSN: 1080-563X 
PUBLISHER: Neva Press 

DOCUMENT TYPE: Journal; General Review 

LANGUAGE: English 

AB A review. Aniracetam is a pyrrolidinone-type cognition enhancer that has 
been clin. used in the treatment of behavioral and psychol . symptoms of 
dementia following stroke and in Alzheimer's disease. New discoveries in 
the behavioral-pharmacol . , biochera. and pharmacokinetics of aniracetam 
provided new indications for this drug in the treatment of various 
central nervous system disorders or diseases. This article 
reviews these new findings and describes the effects of aniracetam in 
various rodent models of mental- function impairment or cerebral 
dysfunction. Also, several metabolites of aniracetam have been reported 
to affect learning and memory in animals. It is, therefore, conceivable 
that major metabolites of aniracetam contribute to its Pharmacol, effects. 
The animal models used in the Pharmacol, evaluation of aniracetam included 
models of hypoattention, hypovigilance-arousal, impulsiveness, 
hyperactivity, fear and anxiety, depression, impaired rapid- eye-movement 
sleep, disturbed temporal regulation, behavioral performance, and bladder 
hyperactivity. These are models of clin. disorders or symptoms that may 
include personality disorders, anxiety, depression, post-traumatic stress 
disorder, attention-def icit/hyperactivity disorder, autism, neg. 
symptoms of schizophrenia, and sleep disorders. At present,, there is no 
convincing evidence that the promising effects of aniracetam in the animal 
models will guarantee its clin. efficacy. It is conceivable, however, 
that clin. trials will demonstrate beneficial effects of aniracetam in the 
above disease states. New findings regarding the mechanism of action of 
aniracetam, its central target sites, and its effects on signal 
transduction are also discussed. • 

REFERENCE COUNT: 103 THERE ARE 103 CITED REFERENCES AVAILABLE FOR 



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=> s central () nervous {) System 
361421 CENTRAL 

25 CENTRALS 
361444 CENTRAL 

(CENTRAL OR CENTRALS) 
192233 NERVOUS 
2184797 SYSTEM 
1202882 SYSTEMS 
2965993 SYSTEM 

(SYSTEM OR SYSTEMS) 
L13 71440 CENTRAL (W) NERVOUS (W) SYSTEM 



=> 53 1X3 ar3d uirinary (> .Ir.contin^sRC©? 
121606 URINARY 

3630 INCONTINENCE? 

1109 URINARY (W) INCONTINENCE? 
L14 37 L13 AND URINARY (W) INCONTINENCE? 



=> s .1.14 Kind review/dt 

1873001 REVIEW/DT 
LI 5 10 LI 4 AND REVIEW/ DT 

=> d 115, xhxh abs, 1-10 



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Text pi^M^; 



ACCESSION NUMBER 
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SOURCE : 



AUTHOR ( S ) 
CORPORATE 

SOURCE : 

PUBLISHER 



DOCUMENT TYPE: 

LANGUAGE : 
AB 



2005: 111657 HCAPLUS 
142:347866 

Pharmacology of the lower urinary tract: basis for 
current and future treatments of urinary incontinence 

Andersson, Karl-Erik; Wain, Alan J. 

Department of Clinical Pharmacology, Lund University 
Hospital, Lund, Swed. 

Pharmacological Reviews (2004), 56(4), 581-631 
CODEN: PAREAQ; ISSN: 0031-6997 

American Society for Pharmacology and Experimental 
Therapeutics 
Journal; General Review 

English 

A review. The lower urinary tract constitutes a functional unit 
controlled by a complex interplay between the central and peripheral 
nervous systems and local regulatory factors. In the adult, micturition 
is controlled by a spinobulbospinal reflex, which is under suprapontine 
control. Several central nervous system transmitters can modulate 
voiding, as well as, potentially, drugs affecting voiding; for example, 
noradrenaline, GABA, or dopamine receptors and mechanisms may be 
therapeutically useful. Peripherally, lower urinary tract function is 
dependent on the concerted action of the smooth and striated muscles of 
the urinary bladder, urethra, and periurethral region. Various 
neurotransmitters, including acetylcholine, noradrenaline, ATP, nitric 
oxide, and neuropeptides, have been implicated in this neural regulation. 
Muscarinic receptors mediate normal bladder contraction as well as at 
least the main part of contraction in the overactive bladder. Disorders 
of micturition can roughly be classified as disturbances of storage or 
disturbances of emptying. Failure to store urine may lead to various 



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forms of incontinence, the main forms of which are urge and stress 
incontinence. The etiol. and pathophysiol . of these disorders remain 
incompletely known, which is reflected in the fact that current drug 
treatment includes a relatively small no. of more or less well-documented 
alternatives. Antimuscarinics are the mainstay of Pharmacol, treatment of 
the overactive bladder syndrome, which is characterized by urgency, 
frequency, and urge incontinence. Accepted drug treatments of stress 
incontinence are currently scarce, but new alternatives are emerging. New 
targets for control of micturition are being defined, but further research 
is needed to advance the pharmacol. treatment of micturition disorders. 
REFERENCE COUNT: 675 THERE ARE 675 CITED REFERENCES AVAILABLE FOR 

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FORMAT 



L15 



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L7\NGUAGE : 
AB 



2005:52316 HCAPLUS 
142:290514 

Therapeutic strategies for urge urinary incontinence 

Steers, William D. 

Department of Urology, University of Virginia Health 
System, Charlottesville, VA, 22908, USA 
Drug Discovery Today: Therapeutic Strategies (2004 )«, 
1(2), 267-273 

CODEN: DDTTC6;. ISSN: 1740-6773 

URL: http : //www. sciencedirect . com/science/iournal/1740 
6773 

B.V. 

General Review; (online computer file) 



Elsevier 
Journal; 

English 

A review. Urinary incontinence and the related disorder overactive 
bladder (OAB) arise from diverse etiologies. Current drug therapies are 
often not curative and are assocd. with prohibitive side effects. New 
therapeutic strategies will go beyond smooth muscle targets to include 
visceral afferents and micturition pathways in the central nervous 
system (CNS) . 

42 THERE ARE 42 CITED REFERENCES AVAILABLE FOR THIS 
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REFERENCE COUNT: 



ANSWER 




ACCESSION NUMBER: 
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AUTHOR (S) : 
CORPORATE SOURCE 



SOURCE : 



PUBLISHER: 
DOCUMENT TYPE: 
LANGUAGE : 
AB A review. 



HCAPLUS COPYRIGHT 2005 ACS on STN 



HCAPLUS 



2004:644185 
142:16872 

Targeting serotonin and norepinephrine receptors in 
stress urinary Incontinence 
Thor, K. B. 

Laboratory of Neurourology, Chief Scientific Officer, 
Dynogen Pharmaceuticals, Inc., Duke University, 
Durham, NC, USA 

International Journal of Gynecology & Obstetrics 
(2004), 86(Suppl. 1), S38-S52 
CODEN: IJGOAL; ISSN: 0020-7292 
Elsevier Ireland Ltd. 
Journal; General Review 
English 

Stress urinary incontinence (SUI) in women is prevalent, 



and there are no globally developed or widely approved drugs for the 
disease. One strategy for improving urinary continence is to augment the 



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function of the urethral rhabdosphincter through neuropharmacol . The 
present review describes the innervation of the urethra, and the role of 
the central nervous system in controlling nerve activity. Targeting 
serotonin and norepinephrine (or noradrenaline) receptors in Onuf's 
nucleus is shown to augment the function of the urethral rhabdosphincter 
by increasing pudendal nerve efferent activity. It is proposed that the 
ability of serotonin and norepinephrine to enhance the effects of 
glutamate (the primary excitatory neurotransmitter for pudendal sphincter 
motor neurons) while having no direct effects of their own, allow 
facilitation of rhabdosphincter activity during urine storage while 
allowing complete relaxation during micturition. Duloxetine, a potent and 
balanced dual serotonin {5-HT) -norepinephrine reuptake inhibitor (SNRI), 
potentiates these physiol. effects of endogenous serotonin and 
norepinephrine (by inhibiting the reuptake of these neurotransmitters in 
the pre-synaptic element) and thereby enhances the central nervous 
system's natural continence control mechanisms. 
REFERENCE COUNT: 47 THERE ARE 47 CITED REFERENCES AVAILABLE FOR THIS 

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L15 ANSWER 4 OF 10 



HCAPLUS COPYRIGHT 2005 ACS on STN 



ACCESSION NUMBER: 2004:479375 HCAPLUS 

DOCUMENT NUMBER: 141:167881 

TITLE: Central nervous system control of the lower 

urinary tract: new pharmacological approaches to 
stress urinary incontinence in women 
Thor, Karl B.; Donatucci, Craig 

Dynogen Pharmaceuticals, Inc. and Division of Urology, 
Department of Surgery, Duke University Medical Center, 

Durham, NC, USA 

Journal of Urology (Hagerstown, MD, United States) 
(2004), 172(1), 27-33 
CODEN: JOURAA; ISSN: 0022-5347 
Lippincott Williams & Wilkins 
Journal; General Review 
English 

A review. Despite the prevalence of stress urinary incontinence in 

women there are no approved drugs for the disease. Designing medical 
therapies requires a comprehensive understanding of how the internal and 
external sphincters are neurol. controlled. In this review recent 
advances in mapping storage and micturition reflexes, and the assocn. of 
serotonergic and noradrenergic systems with these reflexes are discussed. 
Urine storage and micturition are controlled by a series of hard wired 
reflexes that are under the modulatory influence of serotonin and 
norepinephrine. Augmentation of the serotonergic and noradrenergic 
systems with duloxetine increases bladder capacity and urethral 
rhabdosphincter activity. The increase in sphincter activity is mediated 
by al adrenergic receptors and 5-hydroxytryptamine receptors. 
Increasing rhabdosphincter activity with duloxetine may offer a 
therapeutic benefit in women with stress urinary incontinence. 



AUTHOR (S) : 
CORPORATE SOURCE 



SOURCE 



PUBLISHER: 
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LTU^GUAGE : 
AB 



REFERENCE COUNT: 



58 THERE ARE 58 CITED REFERENCES AVAILABLE FOR THIS 
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LIS ANSWER 5 OF 10 HCAPLUS COPYRIGHT 2005 ACS on STN 



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^1 




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2002: 816821 HCAPLUS 
139:16859 

Current and Future Pharmacological Treatment for 



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AUTHOR (S) : 
CORPORATE SOURCE 

SOURCE : 



Overactive Bladder. 

Yoshimura, Naoki; Chancellor, Michael B. 
Dep. Urol., Univ. Pittsburgh Sch. Med., Pittsburgh, 
PA, USA 

Journal of Urology (Hagerstown, MD, United States) 
(2002), 168(5), 1897-1913 
CODEN: JOURAA; ISSN: 0022-5347 
PUBLISHER: Lippincott Williams & Wilkins 

DOCUMENT TYPE: Journal; General Review 

LANGUAGE: English 

AB A review. PURPOSE: Urinary incontinence and overactive bladder are 

important and common conditions that have received little general medical 
attention. The authors reviewed the magnitude and impact of these 
conditions, and discuss pharmacotherapy as well as new drugs under 
investigation. MATERIALS ;\ND METHODS: The main emphasis of this review is 
Pharmacol, therapy for the bladder. The authors discuss currently 
available agents, drugs under development and pharmacol. targets that 
would be suitable targets for treating overactive bladder. Drugs such as 
duloxetine that target not bladder smooth muscle, but rather central 
nervous system control of the micturition reflex are undergoing clin. 
trials. The authors also discuss intravesical therapy and alternative 
drug delivery methods, such as intravesical capsaicin and botulinum toxin, 
with special emphasis on approaches to modulate bladder afferent nerve 
function for preventing overactive bladder. RESULTS: There are many 
advantages to advanced drug delivery systems, including long-term 
therapeutic efficacy, decreased side effects and improved patient 
compliance. Future speculation such as gene therapy holds great promise 
for overactive bladder because it is possible to access all genitourinary 
organs via endoscopy and other minimally invasive techniques that are 
ideally suited for gene therapy. CONCLUSIONS: Traditional anticholinergic 
therapies are limited in their effectiveness. There is great hope for 
future research regarding voiding dysfunction and urinary incontinence 
through a focus on afferent nerve intervention for preventing overactive 
bladder. 

REFERENCE COUNT: 176 THERE ARE 176 CITED REFERENCES AVAILABLE FOR 

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FORMAT 



L15 ANSWER 6 OF 10 HCAPLUS COPYRIGHT 2005 ACS on STN 



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?lB a review examg. 



2002 : 7 64183 HCAPLUS 
138:296900 

Pharmacology and potential therapeutic applications " of 
nitric oxide-releasing nonsteroidal anti-inflammatory 
and related nitric oxide-donating drugs 
Keeble, J. E.; Moore, P. K. 

Centre for Cardiovascular Biology and Medicine, King's 
College, University of London, London, SEl 9RT, UK 
British Journal of Pharmacology (2002), 137(3), 
295-310 

CODEN: BJPCBM; ISSN: 0007-1188 
Nature Publishing Group 
Journal; General Review 

English 

the biol. significance, therapeutic potential and 



mechanism (s) of action of a range of NO-releasing nonsteroidal 
anti-inflammatory drugs (NO-NSAIDs) and related NO-donating drugs (NODDs) 
that are not NSAIDs. The slow release of NO from these compds . leads to 
subtle changes in the profile of Pharmacol, activity of the std. NSAIDs. 



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For example, compared with NSAIDs, NO-NSAIDs have markedly diminished 
gastrointestinal toxicity and improved anti-inflammatory and 
antinociceptive efficacy. In addn., nitroparacetamol exhibits 
hepatoprotection as opposed to the hepatotoxic activity of paracetamol. 
The possibility that NO-NSAIDs or NODDs may be of therapeutic benefit in a 
wide variety of disease states, including pain and inflammation, 
thrombosis and restenosis, neurodegenerative diseases of the central 
nervous system, colitis, cancer, urinary incontinence, liver 
disease, impotence, bronchial asthma and osteoporosis, is discussed. 
REFERENCE COUNT: 145 . THERE ARE 145 CITED REFERENCES AVAILABLE FOR 

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FORMAT 



ANSWER 7 OF 10 HCAPLUS COPYRIGHT 2005 ACS on STN 



ACCESSION NUMBER: 2002:623231 HCAPLUS 

DOCUMENT NUMBER: 137:179283 

TITLE: The tolerability and safety of cholinesterase 

inhibitors in the treatment of dementia 
AUTHOR(S): Inglis, F. 

CORPORATE SOURCE: Glasgow Memory Clinic, Clydebank, UK 

SOURCE: International Journal of Clinical Practice, Supplement 

(2002), 127, 45-63 

CODEN: ICPSFY; ISSN: 1368-504X 
PUBLISHER: Medicom International 

DOCUMENT TYPE: Journal; General Review 

LANGUAGE: English 

AB A review. Cholinesterase inhibitors (ChEls) are dosed in two phases for 
the treatment of dementia, an initial dose-escalation phase to achieve a 
therapeutic dose and a maintenance phase where the therapeutic dose is 
given for long-term therapy. ChEls are assocd. with a range of side 
effects as a result of cholinergic stimulation in different areas of the 
brain and the periphery. Acute, centrally-mediated gastrointestinal 
events (mostly nausea and vomiting) are class effects of all ChEls, and 
are reported mostly during the dose-escalation phase of therapy. These 
events have been assocd. more with the dual acetylcholinesterase/butyrylch 
olinesterase (AChE/BuChE) inhibitor rivastigmine than with the 
AChE-selective inhibitors donepezil and galantamine, probably due to 
rivastigmine ' s higher potency. However, these events can be minimized 
using slow dose escalation with small dose graduations and administration 
with food. Other side effects assocd. with ChEls include central 
nervous system events, extrapyramidal symptoms, sleep disturbances and 
cardiorespiratory events, assocd. with cholinergic activity in the cortex, 
caudate nucleus, brainstem and medulla, resp., and muscle cramps and 
weakness, cardiorespiratory events and urinary incontinence, assocd. 
with peripheral cholinergic activity.' These symptoms are mostly reported 
during the maintenance phase of therapy. They are more frequently 
reported with donepezil, but are rarely reported with rivastigmine, and 
galantamine may not have been marketed long enough to make an adequate 
assessment. These differences are due to the drugs* resp, pharmacol. For 
example, donepezil and rivastigmine are active centrally, in contrast to 
galantamine, which is more active peripherally. Furthermore, rivastigmine 
preferentially inhibits the Gl isoform of cholinesterase, predominantly 
located in the cortex, hippocampus and in neuritic plaques, while 
donepezil and galantamine are not selective for any cholinesterase 
isoforms and have wide cholinergic activity both centrally and 
peripherally. The cholinergic activity of rivastigmine, in contrast to 
donepezil and galantamine, is apparently more targeted at clin. relevant 
brain sites. The pharmacol. profile of rivastigmine results in it having 



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a low potential to interact with other drugs and it may be used with a 
high margin of safety in patients having a wide variety of concomitant 
diseases. Donepezil and galantamine may have significant interactions 
with other drugs that are metabolized by the hepatic cytochrome system and 
therefore need to be used with caution in patients with many concomitant 
illnesses. When dosed with care, ChEls are well tolerated and patient 
compliance and patient and caregiver acceptability are good. The 
favorable tolerability and safety profiles of these agents make them 
suitable first-line therapy for dementia. In addn., patients who have 
tolerability and/or safety problems in maintenance treatment that limit 
the use of donepezil or galantamine may benefit from switching to 
rivastigmine . 

129 THERE ARE 129 CITED REFERENCES AVAILABLE FOR 

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FORMAT 



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2002:38831 HCAPLUS 
137:3845 

Depression and incontinence 
Steers, William D.; Lee, Kyu-Sung 

Department of Urology, University of Virginia Health 
Sciences Center, University of Virginia School of 
Medicine, Charlottesville, VA, 22908, USA 
World Journal of Urology (2001), 19(5), 351-357 
CODEN: WJURDJ; ISSN: 0724-4983 
Springer-Verlag 
Journal; General Review 
English 

A review. The urol. literature suggests that there is an assocn. between 
a- variety of psychiatric disorders and incontinence. Most notably, 
depression is found in a significant percentage of patients with urinary 
incontinence. Depression also occurs in other conditions assocd. with 
urinary urge incontinence, such as aging and dementia, and in neurol . 
disorders such as normal pressure hydrocephalus. Correction of some 
neurol. disorders eliminates both depression and urge incontinence. 
Although chronic medical disorders such as urge incontinence may lead to 
depression, an alternative hypothesis is that these 2 conditions- share a 
common neurochem. pathogenesis. Lowering monoamines such. as serotonin and 
noradrenaline in the central nervous system (CNS) leads to 
depression and urinary frequency and a hyperactive bladder in exptl. 
animals. Thus, depression may not only be the result of persistent 
urinary incontinence, but individuals with altered CNS monoamines 
could manifest both depression and an overactive bladder. The latter 
condition may lead to urge incontinence, urinary frequency, urgency, or 
enuresis. Uncovering further evidence for such a linkage could serve as 
the basis for the development of genetic markers and novel therapeutic 
interventions for these 2 conditions. 

51 THERE ARE 51 CITED REFERENCES AVAILABLE FOR THIS 
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2001:697822 HCAPLUS 
136:363091 

Vanilloid receptor ligands: Hopes and. realities for 
the future 



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AUTHOR(S): Szallasi, Arpad 

CORPORATE SOURCE: Department of Pathology and Immunology, Washington 

University School of Medicine, St Louis, MO, USA 

SOURCE: Drugs & Aging (2001), 18(8), 561-573 

CODEN: DRAGE6; ISSN: 1170-229X 

PUBLISHER: Adis International Ltd. 

DOCUMENT TYPE: Journal; General Review 

LANGUAGE: English 

AB A review. Neurons possessing C-fibers transmit nociceptive information 
into the central nervous system and participate in various reflex 
responses. These neurons carry receptors that bind capsaicin, recently 
identified as the vanilloid VRl receptor. Excitation of these cells by 
capsaicin is followed by a lasting refractory state, termed 
desensitization, in which the neurons fail to respond to a variety of 
noxious stimuli. Desensitization to capsaicin has a clear therapeutic 
potential in relieving neuropathic pain and ameliorating urinary bladder 
overactivity, just to cite 2 important examples. Vanilloids may also be 
beneficial in the treatment of benign prostate hyperplasia (BPH) . Since 
the majority of elderly patients have neuropathic pain co-existent with 
urinary incontinence and/or BPH, a drug that ameliorates pain and 
improves urinary symptoms at the same time promises to be of great clin. 
value in geriatric medicine. In fact, capsaicin has already been shown to 
have a role in the treatment of conditions that can arise in the elderly, 
including herpes zoster-related neuropathic pain, diabetic neuropathy, 
postmastectomy pain, uremic itching assocd. with renal failure, and 
urinary incontinence. The potent VRl agonist resinif eratoxin, now in 
phase II clin. trials, appears to be superior to capsaicin in terms of its 
tolerability profile. Recent discoveries enhance the therapeutic 
potential of vanilloids. The recognition that VRl also functions as a 
principal receptor for protons and eicosanoids implies that VRl 
antagonists may be of value in the treatment of inflammatory hyperalgesia 
and pain. Animal experimentation has already lent support to this 
assumption. The discovery of VRl-expressing cells in the brain as well as 
in non-neural tissues such as the kidney and urothelium places VRl in a 
much broader perspective than peripheral pain perception, and is hoped to 
identify further, yet unsuspected, indications for vanilloid therapy. The 
realization that VRl and cannabinoid CBl receptors have overlapping ligand 
recognition properties may also have far-reaching implications for 
vanilloid therapy. In fact, arvanil, a combined agonist of VRl and CBl 
receptors, has already proved to be a powerful analgesic drug in the 
mouse. From academic mol . biol. labs, to industrial drug discovery 
centers to the clinics, there is a steady flow of new data, forcing us to 
constantly revise the ways the authors are thinking about vanilloid 
receptor ligands and their hopes and realities for the future. This 
review covers the most promising current trends in vanilloid research with 
special emphasis on geriatric medicine. 

REFERENCE COUNT: 95 THERE ARE 95 CITED REFERENCES AVAILABLE FOR THIS 

RECORD. ALL CITATIONS AVAILABLE IN THE RE FORMAT 

L15 ANSWER 10 OF 10 HCAPLUS COPYRIGHT 2005 ACS on STN 



ACCESSION NUMBER: 2001:525684 HCAPLUS 

DOCUMENT NUMBER: 135:237682 

TITLE: Carbon monoxide poisoning: Systemic manifestations and 

complications 
AUTHOR(S): Choi, II Saing 

CORPORATE SOURCE: Department of Neurology, Yonsei University College of 

Medicine, Seoul, 120-752, S. Korea 
SOURCE: Journal of Korean Medical Science (2001), 16(3), 



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253-261 

CODEN: JKMSEH; ISSN: 1011-8934 
PUBLISHER: Korean Academy of Medical Science 

DOCUMENT TYPE: Journal; General Review 

LANGUAGE: English 

AB A review and discussion with 140 refs. CO has the toxic effects of tissue 
hypoxia and produces various systemic and neurol. complications. The main 
clin. manifestations of acute CO poisoning consist of symptoms caused by 
alterations of the cardiovascular system such as initial tachycardia and 
hypertension, and central nervous system symptoms such as headache, 
dizziness, paresis, convulsion, and unconsciousness. CO poisoning also 
produces myocardial ischemia, atrial fibrillation, pneumonia, pulmonary 
edema, erythrocytosis, leukocytosis, hyperglycemia, muscle necrosis, acute 
renal failure, skin lesion, and changes in perception of the visual and 
auditory systems. Of considerable clin. interest, severe neurol. 
manifestations may occur days or weeks after acute CO poisoning. Delayed 
sequelae of CO poisoning are not rare, usually occur in middle or older, 
and are clin. characterized by the symptom triad of mental deterioration, 
urinary incontinence, and gait disturbance. Occasionally, movement 
disorders, particularly parkinsonism, are obsd. In addn., peripheral 
neuropathy following CO poisoning usually occurs in young adults. 

REFERENCE COUNT: 140 THERE ARE 140 CITED REFERENCES AVAILMLE FOR 

THIS RECORD. ALL CITATIONS AVAILABLE IN THE RE 
FORMAT 



=> s 11.3 {) chronic (} obstruct.! ve {) pu.:.TOonary {) disease? 
187986 CHRONIC 

6 CHRONICS 
187990 CHRONIC 

(CHRONIC OR CHRONICS) 

9687 OBSTRUCTIVE 

1 OBSTRUCTIVES 

9688 OBSTRUCTIVE 

(OBSTRUCTIVE OR OBSTRUCTIVES) 
75703 PULMONARY 

2 PULMONARIES 
75703 PULMONARY 

(PULMONARY OR PULMONARIES) 
918183 DISEASE? 

L16 0 L13 (W) CHRONIC (W) OBSTRUCTIVE (W) PULMONARY (W) DISEASE? 

=> -^.og y 

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COST IN U.S. DOLLARS 



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=> file raedline, biosis, eiobasse, hcaplus 
COST IN U.S. DOLLARS 

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Copyright (c) 2005 Elsevier B.V. All rights reserved. 

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USE IS SUBJECT TO THE TERMS OF YOUR STN CUSTOMER AGREEMENT. 

PLEASE SEE " HELP USAGETERMS " FOR DETAILS. 

COPYRIGHT (C) 2005 AMERICAN CHEMICAL SOCIETY (ACS) 

=> venlafaxirje () posr^ () triaxjjaatic {) stress 

LI 0 VENLAFAXINE (W) POST (W) TRAUMATIC (W) STRESS 

=> s vexilaf <utine? {) derivative? 

L2 7 VENLAFAXINE? (W) DERIVATIVE? 

=> d 12 

L2 ANSWER 1 OF 7 BIOSIS COPYRIGHT (c) 2005 The Thomson Corporation on STN 



Ful 


1 ^ 






Tex 


t fe' 







AN 2002:171133 BIOSIS 

DN PREV200200171133 

TI Derivatives of (- ) -venlaf axine and methods of preparing and using the 
same. 

AU Jerussi, Thomas P. [Inventor]; Senanayake, Chrisantha H. [Inventor] 

CS ASSIGNEE: Sepracor, Inc. 

PI US 6342533 20020129 



SINCE FILE TOTAL 
ENTRY SESSION 
0.43 1.69 



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Pages of 24 



so official Gazette of the United States Patent and Trademark Office Patents, 
(Jan. 29, 2002) Vol. 1254, No. 5. http : //www. uspto . qov/web/menu/patdata . ht 
ml . e-file. 

CODEN: 0GUPE7. ISSN: 0098-1133. 
DT Patent 

LA English 

ED Entered STN: 5 Mar 2002 

Last Updated on STN: 4 Apr 2002 



=> d 12, ibib abs, 1-2 

L2 ANSWER 1 OF 7 BIOSIS COPYRIGHT (c) 2005 The Thomson Corporation on STN 



ACCESSION NUMBER 
DOCUMENT NUMBER: 
TITLE: 



2002:171133 BIOSIS 

PREV200200171133 

Derivatives of (-) -venlafaxine and methods of preparing and 
using the same. 

Jerussi, Thomas P. [Inventor]; Senanayake, Chrisantha H. 
[Inventor] 

ASSIGNEE: Sepracor, Inc. 
US 6342533 20020129 

Official Gazette of the United States Patent and Trademark 
Office Patents, (Jan. 29, 2002) Vol. 1254, No. 5. 
http : //www. uspto . qov/web/menu/patdata . html . e-file. 
CODEN: 0GUPE7. ISSN: 0098-1133. 
Patent 
English 

Entered STN: 5 Mar 2002 
Last Updated on STN: 4 Apr 2002 
Methods of preparing, and compositions comprising, derivatives of 
(-) -venlafaxine are disclosed. Also disclosed are methods of treating and 
preventing diseases and disorders including, but not limited to, affective 
disorders such as depression, bipolar and manic disorders, attention 
deficit disorder, attention deficit disorder with hyperactivity, 
Parkinson's disease, epilepsy, cerebral function disorders, obesity and 
weight gain, incontinence, dementia and related disorders. 



AUTHOR (S) : 

CORPORATE SOURCE: 
PATENT INFORMATION: 
SOURCE : 



DOCUMENT TYPE 
LANGUAGE : 
ENTRY DATE: 



AB 



L2 



ANSWER 2 



OF 7 



BIOSIS COPYRIGHT (c) 2005 The Thomson Corporation on STN 



ACCESSION NUMBER 
DOCUMENT NUMBER: 
TITLE: 



2001:391812 BIOSIS 

PREV200100391812 

Derivatives of (+) -venlafaxine and methods of preparing and 
using the same. 

Jerussi, Thomas P. [Inventor]; Senanayake, Chrisantha H. 
[Inventor, Reprint author] 
Shrewsbury, MA, USA 
ASSIGNEE: Sepracor, Inc. 
US 6197828 20010306 

Official Gazette of the United States Patent and Trademark 
Office Patents, (Mar. 6, 2001) Vol. 1244, No. 1. e-file. 
CODEN: 0GUPE7. ISSN: 0098-1133. 
Patent 
English 

Entered STN: 15 Aug 2001 
Last Updated on STN: 23 Feb 2002 
Methods of preparing, . and compositions comprising, derivatives of 
(+) -venlafaxine are disclosed. Also disclosed are methods of treating and 



AUTHOR (S) 



CORPORATE SOURCE: 



PATENT INFORMATION: 
SOURCE : 



DOCUMENT TYPE 
LANGUAGE : 
ENTRY DATE: 



AB 



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preventing diseases and disorders including, but not limited to, affective 
disorders such as depression, bipolar and manic disorders, attention 
deficit disorder, attention deficit disorder with hyperactivity, 
Parkinson's disease, epilepsy, cerebral function disorders, obesity and 
weight gain, incontinence, dementia and related disorders. 



=> d his 

(FILE 'HOME' ENTERED AT 12:05:34 ON 22 NOV 2005) 
FILE 'REGISTRY' ENTERED AT 12:09:17 ON 22 NOV 2005 

FILE 'MEDLINE, BIOSIS, EMBASE, HCAPLUS ' ENTERED AT 12:09:40 ON 22 NOV 2005 
LI OS VENLAFAXINE () POST () TRAUMATIC () STRESS 

L2 7 S VENLAFAXINE? () DERIVATIVE? 

=> s v€3snlaf aKine {) analog? 

L3 1 VENLAFAXINE (W) ANALOG? 

=> d 13 f ibib aiss , 1 

L3 ANSWER 1 OF 1 HCAPLUS COPYRIGHT 2005 ACS on STN 



ACCESSION NUMBER: 
DOCUMENT NUMBER: 
TITLE: 

INVENTOR (S) : 

PATENT ASSIGNEE (S) : 
SOURCE : 

DOCUMENT TYPE: 

LANGUAGE : 

FAMILY ACC. NUM. COUNT: 
PATENT INFORMATION: 



1996:275079 HCAPLUS 
124:333103 

Venlafaxine and related compounds for the treatment of 
hypothalamic amenorrhea in nondepressed women 
Upton, Gertrude V.; Derivan, Albert T.; Rudolph, 
Richard L. 

American Home Products Corp., USA 

U.S., 5 pp . 

CODEN: USXXAM 

Patent 

English 

1 



PATENT NO. 



KIND 



DATE 



APPLICATION NO. 



DATE 



US 


5506270 


A 


19960409 


US 


1995- 


380903 


19950130 


EP 


723779 


Al 


19960731 


EP 


1995- 


309169 


19951218 




R: AT, BE, CH, 


DE, DK, 


ES, FR, 


GB, GR 


• f IE, 


IT, LI, 


LU, NL, PT, SE 


NZ 


280744 


A 


20001124 


NZ 


1995- 


280744 


19951221 


ZA 


9511038 


A 


19970630 


ZA 


1995- 


11038 


19951228 


FI 


9506339 


A 


19960731 


FI 


1995- 


6339 


19951229 


NO 


9505356 


A 


19960731 


NO 


1995- 


5356 


19951229 


AU 


9540752 


Al 


19960808 


AU 


1995- 


40752 


19951229 


AU 


703529 


B2 


19990325 










HU 


75095 


A2 


19970428 


HU 


1995- 


3922 


19951229 


CA 


2167999 


AA 


19960731 


CA 


1996- 


2167999 


19960124 


JP 


08231387 


A2 


19960910 


JP 


1996- 


10850 


19960125 


CN 


1137894 


A 


19961218 


CN 


1996- 


105561 


19960129 


PRIORITY APPLN. INFO.: 






US 


1995- 


380903 


A 19950130 



OTHER SOURCE (S) 
GI 



MARPAT 124:333103 



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AB A method is provided for treating hypothalamic amenorrhea in a 

nondepressed female mammal by administering to the mammal an effective 
amt. of a hydroxycycloalkanephenethyl amine compd. I (A = Q; dotted line = 
optional unsatn.; Rl, R7 = H, alkyl; R2 = alkyl; R4 = H, alkyl, formyl, 
alkanol; R5, R6 = H, OH, alkyl^ alkoxy^ alkanoyloxy, cyano, nitro, 
alkylmercapto, amino, alkylamino, dialkylamino, alkanamido, halo, 
trif luoromethyl, or, taken together, methylene dioxy; n = 0-4) or a 
pharmaceutically acceptable salt thereof. Of particular interest are 
venlafaxine and its pharmaceutically acceptable salts. 



=> d his 

(FILE 'HOME* ENTERED AT 12:05:34 ON 22 NOV 2005) 

FILE 'REGISTRY* ENTERED AT 12:09:17 ON 22 NOV 2005 

FILE 'MEDLINE, BIOSIS, EMBASE, HCAPLUS ' ENTERED AT 12:09:40 ON 22 NOV 2005 

LI OS VENLAFAXINE () POST () TRAUMATIC () STRESS 

L2 7 S VENLAFAXINE? () DERIVATIVE? 

L3 IS VENLAFAXINE () ANALOG? 

=> s 12 and review/dt. 

L4 0 L2 AND REVIEW/DT 

L5 8967 VENLAFAXINE? 

=> senile {) dexaentis or Parkinson -s {) d.lse«ts(»? or epi lepjsi;/? or ?^lzbelxaer? {) dis 
MISMATCHED QUOTE 'PARKINSON'S* 

Quotation marks (or apostrophes) must be used in pairs, 
one before and one after the expression you are setting 
off or masking. 

=> s senile () dementia? or Parkinson? (} diseas<«i? or epilepsy? or AXshelmer? {} dis 
L6 626478 SENILE (W) DEMENTIA? OR PARKINSON? (W) DISEASE? OR EPILEPSY? OR 

ALZHEIMER? (W) DISEASE? OR AMNESIA? OR AMNESIC (W) SYNDROME? OR 

SHY? (W) SYNDROME? OR ANXIETY? 

=> s IS () 15 

L7 12 L6 (W) L5 

=> s 17 and review/dt 

L8 1 L7 AND REVIEW/DT 

=> d IS, ibib ah^, 1 

L8 ANSWER 1 OF 1 HCAPLUS COPYRIGHT 2005 ACS on STN 




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ACCESSION NUMBER: 
DOCUMENT NUMBER: 
TITLE: 



(XR) in the treatment of 



2000:14375 HCAPLUS 
132:44393 

Venlafaxine extended release 
generalized anxiety disorder 
Sheehan, David V. 

Institute for Research in Psychiatry, The University 
of South Florida, Tampa, FL, USA 

Journal of Clinical Psychiatry (1999), 60(Suppl. 22), 

23-28 

CODEN: JCLPDE; ISSN: 0160-6689 
Physicians Postgraduate Press, Inc. 
Journal; General Review 

English 

A review with 2 6 refs. This article reviews results of reports suggesting 
that venlafaxine extended release (XR) may play an important role in the 
treatment of anxiety disorders, particularly generalized anxiety disorder 
(GAD) . Statistically significant improvements in GAD for venlafaxine XR 
compared with placebo on the basis of the Hamilton Rating Scale for 
Anxiety were seen in the acute treatment studies up to 8 wk and were 
maintained for 6 mo. One comparative study found venlafaxine XR to be as 
effective as, or on some measures more effective than, buspirone at 
relieving GAD. Venlafaxine XR was safe and well tolerated in the GAD 
studies, with discontinuation rates due to adverse effects similar to the 
rates seen with placebo or buspirone. 
REFERENCE COUNT: 26 THERE ARE 26 CITED REFERENCES AVAILABLE FOR THIS 

RECORD. ALL CITATIONS AVAILABLE IN THE RE FORMAT 



AUTHOR (S) : 
CORPORATE SOURCE 

SOURCE : 



PUBLISHER: 
DOCUMENT TYPE: 
LANGUAGE : 
AB 



=> s schizophrenia or bordorXine O personality () disorder? 

L9 187794 SCHIZOPHRENIA OR BORDERLINE (W) PERSONALITY (W) DISORDER? 

=> d his 

(FILE •HOME' ENTERED AT 12:05:34 ON 22 NOV 2005) 
FILE 'REGISTRY' ENTERED AT 12:09:17 ON 22 NOV 2005 

FILE 'MEDLINE, BIOSIS, EMBASE, HCAPLUS' ENTERED AT 12:09:40 ON 22 NOV 2005 
LI OS VENLAFAXINE () POST () TRAUMATIC () STRESS 

L2 7 S VENLAFAXINE? () DERIVATIVE? 

L3 IS VENLAFAXINE () ANALOG? 

L4 0 S L2 AND REVIEW/DT 

L5 8967 S VENLAFAXINE? 

L6 626478 S SENILE () DEMENTIA? OR PARKINSON? () DISEASE? OR EPILEPSY? OR 

L7 12 S L6 0 L5 

L8 1 S L7 AND REVIEW/DT 

L9 187794 S SCHIZOPHRENIA OR BORDERLINE () PERSONALITY () DISORDER? 

=> s 19 {) 15 

LIO 1 L9 (W) L5 

=> js 110 and revxew/dt 

Lll 0 LIO AND REVIEW/DT 

=> s cocaine () addiction or alcohol <) addiction? 

L12 4026 COCAINE (W) ADDICTION OR ALCOHOL (W) ADDICTION? 

=> s 112 {) 15 

LIS 0 L12 (W) L5 



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=> s 112 and 15 

L14 9 L12 AND L5 

=> s 114 and review/dt 

LI 5 0 LI 4 AND REVIEW/ DT 

=> s buLintia. () nervosa? or Gllles? (} toxsrette {) syndro?n© or vasocaotor {) flushirsg 
L16 16028 BULIMIA (W) NERVOSA? OR GILLES? (W) TOURETTE (W) SYNDROME OR ' 

VASOMOTOR (W) FLUSHING? OR CHRONIC (W) FATIGUE (W) SYNDROME? 

=> s 116 () 15 

L17 0 L16 (W) L5 

=> s 116 and 15 

L18 66 L16 AND L5 

=> s 118 arad rav.iex<?/dt 

LI 9 4 LI 8 AND REVIEW/DT 

=> d 119, iblb afos, 1-4 

LI 9 ANSWER 1 OF 4 MEDLINE on STN 



ACCESSION NUMBER 
DOCUMENT NUMBER: 
TITLE: 
AUTHOR: 



2003366271 MEDLINE 
PubMed ID: 12900988 

Pharmacologic treatment of binge eating disorder. 
Carter William P; Hudson James I; Lalonde Justine K; 
Pindyck Lindsay; McElroy Susan L; Pope Harrison G Jr 
Biological Psychiatry Laboratory, McLean Hospital, Belmont, 
MA 02478, USA. . wpcarter@partners . org 
T32 DA 07252 (NIDA) 

International journal of eating disorders, (2003) 34 Suppl 
S74-88. Ref: 50 

Journal code: 8111226. ISSN: 0276-3478. 
United States 

Journal; Article; (JOURNAL ARTICLE) 
Greneral Review; (REVIEW) 

English 

Priority Journals 
200312 

Entered STN: 20030806 
Last Updated on STN: 20031224 
Entered Medline: 20031223 
OBJECTIVE: To review the findings from pharmacologic trials of binge 
eating disorder (BED) and to provide guidelines for pharmacologic 
treatment. METHODS: The literature was searched for studies of 
pharmacologic treatment of BED and related conditions, such as nonpurging 
bulimia nervosa. RESULTS: Placebo-controlled studies of desipramine, 
fluvoxamine, fluoxetine, sertraline, citalopram, dexf enf luramine, 
sibutramine, and topiramate have demonstrated the efficacy of these agents 
in the treatment of BED. An open trial of venlafaxine has offered 
preliminary evidence for the efficacy of this medication. Guidelines for 
pharmacologic management of BED are provided. CONCLUSIONS: The literature 
offers support for the use of agents from three categories of medication 
(antidepressants, appetite suppressants, and anticonvulsants) in the 
treatment of BED. 

Copyright 2003 by Wiley Periodicals, Inc. 



CORPORATE SOURCE: 

CONTRACT NUMBER: 
SOURCE : 



PUB . COUNTRY : 
DOCUMENT TYPE 

LANGUAGE : 
FILE SEGMENT: 
ENTRY MONTH: 
ENTRY DATE: 



AB 



LI 9 ANSWER 2 OF 4 



MEDLINE on STN 



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ACCESSION NUMBER 
DOCUMENT NUMBER: 
TITLE: 
COMMENT : 



: 829-30. 



AUTHOR: 
CORPORATE 

SOURCE : 



SOURCE : 



2000387069 MEDLINE 
PubMed ID: 10926050 

New indications for antidepressants. 
Comment in: J Clin Psychiatry. 200.1 Oct; 62 (10) 
PubMed ID: 11816876 
Schatzberg A F 

Department of Psychiatry and Behavioral Sciences, Stanford 
University School of Medicine, Calif 94305-5548, USA. 
Journal of clinical psychiatry, (2000) 61 Suppl 11 9-17. 
Ref: 73 

Journal code: 7801243. ISSN: 0160-6689. 
United States 

Journal; Article; (JOURNAL ARTICLE) 
General Review; (REVIEW) 

(REVIEW, TUTORIAL) 
English 

Priority Journals 

200008 

Entered STN: 20000818 
Last Updated on STN: 20020426 
Entered Medline: 20000804 
The second and third generation of antidepressants, i.e., the selective 
serotonin reuptake inhibitors, nefazodone, venlafaxine, and mirtazapine, 
are proving to be useful in a variety of seemingly diverse disorders, 
including most anxiety disorders. In addition to receiving approval from 
the U.S. Food and Drug Administration (FDA) for major depressive 
disorder, some of the newer antidepressants have received FDA approval for 
other disorders, e.g., generalized anxiety disorder (venlafaxine), 
bulimia nervosa (fluoxetine), obsessive-compulsive disorder 
(f luvoxamine, paroxetine, sertraline, and fluoxetine) , social phobia 
(paroxetine), panic disorder (sertraline, paroxetine), and posttraumatic 
stress disorder (sertraline) . In controlled studies, these agents have 
also shown usefulness in premenstrual dysphoric disorder, borderline 
personality disorder, obesity, smoking cessation, and alcoholism. This 
article describes the new and potential indications for recently developed 
antidepressants and the studies that suggested these indications. 



PUB. COUNTRY: 
DOCUMENT TYPE 



LANGUAGE : 
FILE SEGMENT 
ENTRY MONTH: 
ENTRY DATE: 



AB 



L19 ANSWER 3 OF 4 HCAPLUS COPYRIGHT 2005 ACS on STN 



HCAPLUS 



ACCESSION NUMBER 
DOCUMENT NUMBER: 
TITLE: 
AUTHOR (S) : 
CORPORATE SOURCE 



SOURCE 



PUBLISHER: 
DOCUMENT TYPE 
LANGUAGE : 
AB 



2000:596373 

134: 65678 

New indications for antidepressants 
Schatzberg, Alan F. 

Department of Psychiatry and Behavioral Sciences, 
Stanford University School of Medicine, Stanford, CA, 
94305-5548, USA 

Journal of Clinical Psychiatry (2000), 61 (Suppl. 11), 
9-17 

CODEN: JCLPDE; ISSN: 0160-6689 
Physicians Postgraduate Press, Inc. 
Journal; General Review 
English 

A review with 73 refs. The second and third generation of 
antidepressants, i.e., the selective serotonin reuptake inhibitors, 
nefazodone, venlafaxine, and mirtazapine, are proving to be useful in a 
variety of seemingly diverse disorders, including most anxiety disorders. 
In addn. to receiving approval from the U.S. Food and Drug Administration. 



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(FDA) for major depressive disorder, some of the newer antidepressants 
have received FDA approval for other disorders, e.g., generalized anxiety 
disorder (venlafaxine) ^ bulimia nervosa (fluoxetine), 

obsessive-compulsive disorder ( f luvoxamine, paroxetine, sertraline, and 
fluoxetine), social phobia (paroxetine), panic disorder (sertraline, 
paroxetine), and posttraumatic stress disorder (sertraline). In 
controlled studies, these agents have also shown usefulness in 
premenstrual dysphoric disorder, borderline personality disorder, obesity, 
smoking cessation, and alcoholism. This article describes the new and 
potential indications for recently developed antidepressants and the 
studies that suggested these indications. 
REFERENCE COUNT: 73 THERE ARE 73 CITED REFERENCES AVAILABLE FOR THIS 

RECORD. ALL CITATIONS AVAILABLE IN THE RE FORMAT 



L19 ANSWER 4 OF 4 HCAPLUS COPYRIGHT 2005 ACS on STN 




ACCESSION NUMBER: 1998:469364 HCAPLUS 

DOCUMENT NUMBER: 129:239318 

TITLE: Potential applications of venlafaxine 

AUTHOR(S): Nutt, D.; Johnson, F. Neil 

CORPORATE SOURCE: School of Medical Sciences, University of Bristol, 

Bristol, BS8 ITD, UK 
SOURCE: Reviews in Contemporary Pharmacotherapy (1998), 9(5), 

321-331 

CODEN: RCPHFW; ISSN: 0954-8602 
PUBLISHER: Marius Press 

DOCUMENT TYPE: Journal; General Review 

LANGUAGE: English 

AB A review with 95 refs. The action of venlafeucine on at least two 

neurotransmitter systems suggests that this agent may have potential 
applications in a variety of conditions in addn. to the treatment of 
depression. Evidence on the point is relatively scanty at the present 
time, but such information as is available suggests that venlafaxine may 
have a future role in the management of several psychiatric conditions. 
These include: obsessive-compulsive disorder; panic disorder; attention 
deficit hyper-activity disorder (in children and in adults); borderline 
personality disorder; chronic fatigue syndrome; and possibly loss of 
libido and/or erectile dysfunction. There are also suggestions of 
therapeutic benefit arising from venlafaxine treatment of phobic 
conditions, specifically agoraphobia and social phobia. Recent work 
indicates that venlafaxine may reduce anxiety concomitant with 
depressive symptoms as well as anxiety occurring in the absence of 
depression, and that it may be rather more effective in doing so than is 
the case for several comparator agents. Venlafaxine appears to be 
effective in treating certain forms of pain; this is particularly evident 
against some types of headache, and there are indications of efficacy also 
against postherpetic neuralgia, chronic radicular back pain, and 
fibromyalgia. While venlafaxine has been found to show some degree of 
efficacy against Raynaud's phenomenon, it is unlikely to be better than 
selective serotonin reuptake inhibitors in the treatment of this 
condition. Further studies of venlafaxine are likely to reveal a wider 
spectrum of potential applications for this agent. 

REFERENCE COUNT: 95 THERE ARE 95 CITED REFERENCES AVAIL7\BLE FOR THIS 

RECORD. ALL CITATIONS AVAILABLE IN THE RE FORMAT 



=> d his 

(FILE 'HOME* ENTERED AT 12:05:34 ON 22 NOV 2005) 



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FILE 'REGISTRY' ENTERED AT 12:09:17 ON 22 NOV 2005 

FILE 'MEDLINE, BIOSIS, EMBASE, HCAPLUS ' ENTERED AT 12:09:40 ON 22 NOV 2005 



LI 


0 


S 


VENLAFAXINE () POST () TRAUMATIC () STRESS 


L2 


7 


s 


VENLAFAXINE? {) DERIVATIVE? 


L3 


1 


s 


VENLAFMINE ( ) ANALOG? 


L4 


0 


s 


L2 AND REVIEW/DT 


L5 


8967 


s 


VENLAFAXINE? 


L6 


626478 


s 


SENILE 0 DEMENTIA? OR PARKINSON? () DISEASE? 


L7 


12 


s 


L6 0 L5 


L8 


1 


s 


L7 AND REVIEW/DT 


L9 


187794 


s 


SCHIZOPHRENIA OR BORDERLINE () PERSONALITY () 


LIO 


1 


s 


L9 0 L5 


Lll 


0 


s 


LIO AND REVIEW/DT 


L12 


4026 


s 


COCAINE 0 ADDICTION OR ALCOHOL {) ADDICTION? 


L13 


0 


s 


L12 0 L5 


L14 


9 


s 


L12 AND L5 


L15 


0 


s 


LI 4 AND REVIEW/DT 


L16 


16028 


s 


BULIMIA 0 NERVOSA? OR GILLES? () TOURETTE {) 


L17 


0 


s 


L16 0 L5 


L18 


66 


s 


LI 6 AND L5 


L19 


4 


s 


LI 8 AND REVIEW/DT 



OR EPILEPSY? OR 



DISORDER? 



SYNDROME OR VAS 



=> s IS aad urinary {) iiicontirience? 

L20 36 L5 AND URINARY (W) INCONTINENCE? 

=> a 120 arjd rav.i.ev?/dt 

A IS NOT A RECOGNIZED COMMAND 

The previous command name entered was not recognized by the system. 
For a list of commands available to you in the current .file, enter 
" HELP COMMANDS " at an arrow prompt (=>) . 

=> s 120 and review/dt 

L21 1 L20 AND REVIEW/DT 

=> d 121, ibib abs^ 1 

ANSWER 1 OF 1 HCAPLUS COPYRIGHT 2005 ACS on STN 




ACCESSION NUMBER: 2004:405479 HCAPLUS 

DOCUMENT NUMBER: 141:46634 
TITLE: Other antidepressants 

AUTHOR(S): Preskorn, S. H.; Ross, R. 

CORPORATE SOURCE: Department of Psychiatry and Behavioral Sciences, 

Psychiatric Research Institute, University of Kansas 
School of Medicine, Wichita, KS, KA 67214, USA 

SOURCE: Handbook of Experimental Pharmacology (2004), 

157 (Antidepressants) , 263-324 
CODEN: HEPHD2; ISSN: 0171-2004 

PUBLISHER : Springer-Verlag 

DOCUMENT TYPE: Journal; General Review 

LANGUAGE: English 

AB A review. This chapter reviews the following antidepressants, which do 
not belong to one of the major classes described in the three preceding 
chapters: bupropion, mirtazapine and mianserin, nefazodone and trazodone, 
reboxetine, venlafaxine, duloxetine, milnacipran, and tianeptine. 
Unlike the selective serotonin reuptake inhibitors (SSRIs) , many of these 
antidepressants have an ascending rather than a flat dose-response curve. 



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The chapter provides a brief review of the chem. , pharmacol., metab., 
safety and adverse effects, clin. use, and therapeutic indications of each 
antidepressant. Bupropion is a weak dual uptake inhibitor of both 
dopamine and norepinephrine (NE) . Information concerning its 
pharmacodynamic and pharmacokinetic properties is limited, primarily 
because of the age of the drug (clin. trials begun in the mid-1970s) . 
Bupropion's most serious side effect is dose-dependent seizures, so that 
the highest recommended doses are 450 and 400 mg/day for the immediate 
release (IR) and sustained release (SR) formulations, resp. Other adverse 
effects include restlessness, activation, tremors, insomnia, and nausea. 
Bupropion was found to be an effective antidepressant in several 
double-blind studies that generally used doses higher than the max. 
recommended dose of 450 mg/day. Despite fairly modest evidence of 
antidepressant efficacy, bupropion may be useful in a no. of clin. 
situations, including for patients with prominent psychomotor retardation, 
Parkinson's disease, or attention-def icit/hyperactivity disorder; for 
patients who have failed to respond to other antidepressants; and for 
patients who cannot tolerate sexual side effects of other antidepressants. 
Bupropion has also been approved as an aid in smoking cessation. 
Mirtazapine and its forerunner mianserin, are tetracyclic compds . with a 
unique mechanism of action. Mirtazapine is an a2-antagonist that 
increases noradrenergic and serotonergic neurotransmission, the primary 
mechanism thought to underlie its antidepressant activity. Mirtazapine 
does not cause many of the side effects assocd. with the SSRIs (e.g., 
nausea, loose stools, disturbed sleep pathol., sexual dysfunction) and 
causes minimal anticholinergic effects, no quinidine-like effects, and no 
effects on blood pressure. Sedation can be a problem, esp. early in 
treatment, although this may be an advantage for patients with prominent 
insomnia, anxiety, or agitation. Mirtazapine can cause increased appetite 
and wt. gain, transient neutropenia, and transient mild elevations of 
liver function tests. Three cases of agranulocytosis were reported out of 
3,000 patients in the mirtazapine clin. trial program, an incidence too 
low to draw any conclusion about cause and effect. Although postmarketing 
experience has not found an unusual no. of cases of agranulocytosis, the 
package insert in the United States contains a warning that a white blood 
cell count should be done if a patient taking mirtazapine develops signs 
of fever or infection. Because of its unique mechanism of action, 
mirtazapine may be efficacious for patients who have not benefited from 
other types of antidepressants. Nefazodone and trazodone have chem. 
related structures that incorporate 5-HT2A receptor blockade plus weak 
5-HT uptake blockade and possibly NE uptake blockade. Trazodone is widely 
used as a nonhabit-f orming sleep aid rather than as an antidepressant. 
The antihistaminergic properties of trazodone are partly responsible for 
its popularity as a sleep aid, but can cause significant problems with 
daytime sedation when it is used as an antidepressant; however, it may be 
useful for treating agitation in geriatric patients. Nefazodone, a more 
potent serotonin re-uptake inhibitor (SRI) than trazodone, was designed 
with the goal of producing a better antidepressant than trazodone, 
although it is a much weaker SRI than the SSRIs or venlafaxine. Because 
it substantially inhibits CYP 3A3/4, nefazodone can elevate levels of 
coprescribed drugs metabolized via CYP 3A/3/4. Nefazodone produces less 
activation and sexual dysfunction than the SSRIs and venlafaxine; it 
does not cause blood pressure elevation or disturb sleep physiol.; it 
improves subjective sleep quality. The incidence and severity of the 
following adverse effects increase in a dose-dependent fashion as a 
function of the starting dose of nefazodone: dizziness/lightheadedness, 
confusion, sedation, gastrointestinal side effects. Nefazodone appears to 
have efficacy in patients with clin. depression and prominent anxiety. 
Although there appears to be greater interpatient variability in response 
to nefazodone than to many of the other newer antidepressants, nefazodone 



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can be a useful option for patients who are unable to tolerate the adverse 
effects of the SSRIs. Reboxetine is a selective NE reuptake pump 
inhibitor. Its most common adverse effects are insomnia, sweating, 
constipation, dry mouth, and urinary hesitancy. Most of the published 
trials of reboxetine have been active rather than placebo-controlled and 
results were not published in full with rigorous peer review, compromising 
the ability to make an assessment of efficacy. Sufficient evidence of the 
efficacy of reboxetine in major depression has not been presented to 
receive approval for marketing in the United States, but reboxetine is 
available in several other countries. Venlafaxine, a phenylethylamine, 
first inhibits the neuronal uptake pump for serotonin (SE) and then at 
higher concns. inhibits the uptake pump for NE. Unlike tertiary amine 
tricyclic antidepressants (TCAs) , which also inhibit the SE and NE uptake 
pumps, venlafaxine has low affinity for most other neural receptors and 
does not inhibit sodium fast channels, making it relatively safe in 
overdose. Its adverse effects change qual. as the dose increases because 
of progressively greater blockade of NE uptake with increasing doses. At 
low doses, the adverse-effect profile is similar to an SSRI with nausea, 
loose stools, sexual dysfunction, while venlafaxine at higher doses can 
produce generally mild increases in blood pressure, diaphoresis, 
tachycardia, tremors, and anxiety. A disadvantage of venlafaxine 
relative to the SSRIs is the potential for dose-dependent blood pressure 
elevation, most likely due to the NE uptake inhibition caused by higher 
doses; however, this adverse effect is infrequently obsd. at doses below 
225 mg/day. Venlafaxine and the SSRIs have similar advantages over the 
TCAs and monoamine oxidase inhibitors. Venlafaxine also has a no. of 
potential advantages over the SSRIs, including an ascending 
dose-antidepressant response curve, with possible greater overall efficacy 
at higher doses, evidence of more rapid onset of antidepressant action, 
evidence of superior efficacy in hospitalized patients with major 
depressive disorder compared with placebo or fluoxetine, and minimal 
effects on GYP enzymes in contrast to fluoxetine, fluvoxamine, paroxetine, 
and the non-SSRI, bupropion. Duloxetine is a SE-NE re-uptake pump 
inhibitor, which is pending approval in the United States and other 
countries in late 2003. It will be the third member of this Pharmacol, 
class, which also contains venlafaxine and milnacipran ( sibutramine, the 
fourth member of this class, is marketed for obesity rather than major 
depression) . Only a limited no. of articles have been published on this 
compd. but more should be expected shortly after its market introduction. 
The manufacturer is initially seeking indications for both major 
depression and urinary incontinence. Due to its inhibition of the SE 
and NE uptake pumps, duloxetine will undoubtedly carry a warning against 
use in combination with monoamine oxidase inhibitors. It is also a 
moderate inhibitor of GYP 2D6, so that modest dose redns . and careful 
monitoring will be needed when prescribing duloxetine in combination with 
drugs that are preferentially metabolized by GYP 2D6, particularly those 
with narrow therapeutic indexes. The most common side effects identified 
in clin. trials to date appear to be nausea, dry mouth, dizziness, 
constipation, insomnia, asthenia, and hypertension, consistent with its 
mechanisms of action. Clin, trials to date have demonstrated rates of 
response and remission in patients with major depression that are 
comparable to other marketed antidepressants reviewed in this book. 
Although milnacipran is marketed in France, Japan, and a few other 
countries, its development in the United States was discontinued. It is 
an SE and NE reuptake inhibitor in the same class as venlafaxine, 
duloxetine, and the anti-obesity drug, sibutramine. Milnacipran would be 
predicted to be susceptible to the same pharmacodynamic drug-drug 
interactions as other drugs in this class, but would not be expected to be 
involved in any GYP enzyme-mediated drug-drug interactions. Milnacipran 
at doses of 50-200 mg/day has a favorable adverse-effect profile when 



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Page 13 of 24 



compared with tertiary amine TCAs, including a lower incidence of abnormal 
liver function tests. At doses of 50 or 100 mg twice a day but not 100 mg 
once a day, it caused a lower incidence of nausea and anxiety but a higher 
incidence of headache, dry mouth, and dysuria than did fluoxetine, 20 
mg/day, or fluvoxamine, 100 mg twice a day. As with other drugs in this 
class, dysuria is the most common troublesome and dose-dependent adverse 
effect (occurring in up to 7% of patients) . High-dose milnacipran has 
been reported to cause blood pressure elevation. Like reboxetine, most of 
the published trials of milnacipran have been active rather than 
placebo-controlled and results were not published in full with rigorous 
peer review, compromising the ability to make an assessment of efficacy; 
however, findings to date suggest that milnacipran produces a superior 
antidepressant response compared with placebo at doses of 50 and 100 mg 
twice a day. Tianeptine is marketed in France but few other countries 
around the world and there is little knowledge of this drug in the United 
States and other English-speaking countries. However, a surprising amt. 
of research, particularly preclin., has been done with tianeptine, in part 
because of its apparent novel mechanism of action: Tianeptine, in contrast 
to most other antidepressants, increases SE uptake into neurons rather 
than blocking it. However, its side-effect profile is similar to that of 
other newer antidepressants, with low abuse potential and a low risk of 
adverse effects on the cardiovascular system, the cholinergic systems, 
sleep/arousal, cognition, psychomotor functioning, and wt . The most 
common adverse effects include nausea, constipation, abdominal pain, 
headache, dizziness, and altered dreaming. Hepatotoxicity has been 
reported but is rare. Like reboxetine and milnacipran, most of the 
published trials of tianeptine have been active rather than 
placebo-controlled and results were not published in full with rigorous 
peer review, compromising the ability to assess efficacy; however, trials 
to date do suggest efficacy in patients with major depression. 
REFERENCE COUNT: 279 THERE ARE 279 CITED REFERENCES AVAILABLE FOR 

THIS RECORD. ALL CITATIONS AVAILABLE IN THE RE 

FORMAT 



-> s central <) nervous {) system? {) disorder? 

L22 3134 CENTRAL (W) NERVOUS (W) SYSTEM? (W) DISORDER? 

=> s 122 and urinary () inccntin<c-nce'? 

L23 18 L22 AND URINARY (W) INCONTINENCE? 

=> .«i 123 and roview/dt 

L24 1 L23 AND REVIEW/ DT 



=> d 124, ±h±h i 

L24 ANSWER 1 OF 1 



ACCESSION NUMBER: 

DOCUMENT NUMBER: 

TITLE: 

AUTHOR: 

SOURCE : 

PUB. COUNTRY: 
DOCUMENT TYPE: 

LANGUAGE : 
FILE SEOyiENT: 



MEDLINE on STN 







Tex 





77039644 MEDLINE 
PubMed ID: 790743 

Nomenclature of neurogenic bladder. 
Gibbon N O 

Urology, (1976 Nov) 8 (5) 423-31. Ref: 
Journal code: 0366151. ISSN: 0090-4295. 
United States 

Journal; Article; (JOURNAL ARTICLE) 
General Review; (REVIEW) 

English 

Priority Journals 



29 



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ENTRY MONTH: 197612 

ENTRY DATE: Entered STN: 19900313 

Last Updated on STN: 19990129 
Entered Medline: 19761223 

AB Vesicourethral physiology is reviewed briefly in the light of recent 
developments. The effect on bladder function of central nervous 
system disorders is considered and attention is drawn to the 
desirability of diverting interest from the bladder to the urethra in 
neuropathic cases. It is concluded that there are only two basic types of 
neuropathic bladder function — in lesions of and above the sacral reflex 
pathways, respectively. Neurologically these are classified according to 
the condition of the anal and bulbocavernosus reflexes and the ice water 
test. 



=> s chronic (> obstructive () pulmonary {) disease? 

L25 37137 CHRONIC (W) OBSTRUCTIVE (W) PULMONARY (W) DISEASE? 

=> d his 

(FILE 'HOME* ENTERED AT 12:05:34 ON 22 NOV 2005) 
FILE 'REGISTRY' ENTERED AT 12:09:17 ON 22 NOV 2005 

FILE 'MEDLINE, BIOSIS, EMBASE, HCAPLUS ' ENTERED AT 12:09:40 ON 22 NOV 2005 



LI 


0 


S 


VENLAFAXINE () POST () TRAUMATIC () STRESS 


L2 


7 


S 


VENLAFAXINE? () DERIVATIVE? 


L3 


1 


S 


VENLAFAXINE ( ) ANALOG? 


L4 


0 


S 


L2 AND REVIEW/ DT 


L5 


8967 


S 


VENLAFAXINE? 


L6 


626478 


s 


SENILE 0 DEMENTIA? OR PARKINSON? () DISEASE? OR EPILEPSY? OR 


L7 


12 


s 


L6 0 L5 


L8 


1 


s 


L7 AND REVIEW/DT 


L9 


187794 


S 


SCHIZOPHRENIA OR BORDERLINE () PERSONALITY () DISORDER? 


LIO 


1 


s 


L9 0 L5 


Lll 


0 


s 


LIO AND REVIEW/DT 


L12 


4026 


s 


COCAINE 0 ADDICTION OR ALCOHOL () ADDICTION? 


L13 


0 


s 


L12 0 L5 


L14 


9 


s 


L12 AND L5 


L15 


0 


s 


L14 AND REVIEW/DT 


L16 


16028 


s 


BULIMIA 0 NERVOSA? OR GILLES? () TOURETTE () SYNDROME OR VAS 


L17 


0 


s 


L16 0 L5 


L18 


66 


s 


L16 AND L5 


L19 


4 


s 


L18 AND REVIEW/DT 


L20 


36 


s 


L5 AND URINARY () INCONTINENCE? 


L21 


1 


s 


L20 AND REVIEW/DT 


L22 


3134 


s 


CENTRAL {) NERVOUS () SYSTEM? () DISORDER? 


L23 


18 


s 


L22 AND URINARY () INCONTINENCE? 


L24 


1 


s 


L23 AND REVIEW/DT 


L25 


37137 


s 


CHRONIC 0 OBSTRUCTIVE () PULMONARY () DISEASE? 



=> ,«i 125 «TLnd 15 

L26 1 L25 AND L5 

=> s 126 and review/dt 

L27 0 L26 AND REVIEW/DT 

=> s 15 arid pain? 

L28 780 L5 AND PAIN? 



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=> s 15 0 pain 

L29 ' 3 L5 (W) PAIN 

=> js 129 and revlew/dt 

L30 1 L29 AND REVIEW/DT 

=> d 130, .ibil> abs, 1 

L30 ANSWER 1 OF 1 HCAPLUS COPYRIGHT 2005 ACS on STN 



^ Full ■ 






Text 







ACCESSION NUMBER 
DOCUMENT NUMBER: 
TITLE: 
AUTHOR (S) : 
CORPORATE SOURCE 

SOURCE : 



PUBLISHER: 
DOCUMENT TYPE: 
LANGUAGE : 
AB A review. 



2002 : 580046 HCAPLUS 
137:149663 

Antidepressants in pain management 
Carter, Gregory T.; Sullivan, Mark D. 
Department of Rehabilitation Medicine, University of 
Washington School of Medicine, Seattle, WA, 98195, USA 
Current Opinion in Investigational Drugs (PharmaPress 
Ltd.) (2002), 3(3), 454-458 
CODEN: COIDAZ; ISSN: 1472-4472 
PharmaPress Ltd. 
Journal; General Review 
English 

Antidepressants exhibit a no. of Pharmacol, mechanisms, 



including norepinephrine and serotonin modulation, direct and indirect 
effects on opioid receptors, inhibition of histamine, cholinergic and 
N-methyl-D-aspartate receptors, and inhibition of ion channel activity. 
Although it is not entirely clear which mechanisms produce analgesia and 
to what extent, the available animal and clin. trials data indicates that 
tricyclic antidepressants are effective in treating many types of pain. 
The newer selective serotonin reuptake inhibitors also appear to be 
effective for chronic headache and other non-neuropathic forms of chronic 
pain but are not as well studied. This article reviews the current basic 
and clin. research on antidepressants in pain management. 
REFERENCE COUNT: 59 THERE ARE 59 CITED REFERENCES AVAILABLE FOR THIS 

RECORD. ALL CITATIONS AVAILABLE IN THE RE FORMAT 



=> d his 

(FILE 'HOME* ENTERED AT 12:05:34 ON 22 NOV 2005) 
FILE 'REGISTRY' ENTERED AT 12:09:17 ON 22 NOV 2005 

FILE 'MEDLINE, BIOSIS, EMBASE, HCAPLUS' ENTERED AT 12:09:40 ON 22 NOV 2005 



LI OS VENLAFAXINE () POST () TRAUMATIC () STRESS 

L2 7 S VENLAFAXINE? () DERIVATIVE? 

L3 IS VENLAFAXINE () ANALOG? 

L4 0 S L2 AND REVIEW/DT 

L5 8967 S VENLAFAXINE? 

L6 626478 S SENILE () DEMENTIA? OR PARKINSON? () DISEASE? OR EPILEPSY? OR 

L7 12 S L6 0 L5 

L8 1 S L7 AND REVIEW/DT 

L9 187794 S SCHIZOPHRENIA OR BORDERLINE () PERSONALITY () DISORDER? 

LIO 1 S L9 0 L5 

Lll 0 S LIO AND REVIEW/DT 

L12 4026 S COCAINE () ADDICTION OR ALCOHOL () ADDICTION? 

L13 0 S L12 0 L5 

L14 9 S L12 AND L5 

L15 0 S L14 AND REVIEW/DT 



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and fibromyalgia, can be challenging for primary care providers to treat. 
Antidepressants that block reuptake of both serotonin and norepinephrine, 
such as the tricyclic antidepressants (e.g., amitriptyline) , have been 
used to treat pain syndromes in patients with or without comorbid MDD or 
GAD. Venlafaxine, a serotonin and norepinephrine reuptake inhibitor, 
has been safe and effective in animal models, healthy human volunteers, 
and patients for treatment of various pain syndromes. The use of 
venlafaxine for treatment of pain associated with MDD or GAD, 
neuropathic pain, headache, fibromyalgia, and postmastectomy pain syndrome 
is reviewed. Currently, no antidepressants, including venlafaxine, are 
approved for the treatment of chronic pain syndromes. Additional 
randomized, controlled trials are necessary to fully elucidate the role of 
venlafaxine in the treatment of chronic pain. 



ANSWER 




ACCESSION NUMBER: 
DOCUMENT NUMBER: 
TITLE: 
AUTHOR (S) : 
CORPORATE SOURCE: 



HCAPLUS COPYRIGHT 2005 ACS on STN 



HCAPLUS 



SOURCE : 

PUBLISHER: 
DOCUMENT TYPE: 
L7\NGUAGE : 
AB 



2004:583658 
141:184422 

Treatment of pain syndromes with venlafaxine 
Grothe, Dale R.; Scheckner, Brian; Albano, Dominick 
Global Medical Communications, Neuroscience, Wyeth 
Pharmaceuticals, Collegeville, PA, USA 
Pharmacotherapy (2004), 24(5), 621-629 
CODEN: PHPYDQ; ISSN: 0277-0008 
Pharmacotherapy Publications 
Journal; General Review 
English 

A review. Major depressive disorder (MDD) and anxiety disorders such as 
generalized anxiety disorder (GAD) are often accompanied by chronic 
painful symptoms. Examples of such symptoms are backache, headache, 
gastrointestinal pain, and joint pain. In addn., pain generally not 
assocd. with major depression or an anxiety disorder, such as peripheral 
neuropathic pain (e.g., diabetic neuropathy and postherpetic 
neuralgia) , cancer pain, and fibromyalgia, can be challenging for 
primary care providers to treat. Antidepressants that block reuptake of 
both serotonin and norepinephrine, such as the tricyclic antidepressants 
(e.g., amitriptyline), have been used to treat pain syndromes in patients 
with or without comorbid MDD or GAD. Venlafaxine, a serotonin and 
norepinephrine reuptake inhibitor, has been safe and effective in animal 
models, healthy human volunteers, and patients for treatment of various 
pain syndromes. The use of venlafaxine for treatment of pain assocd. 
with MDD or GAD, neuropathic pain, headache, fibromyalgia, and 
postmastectomy pain syndrome is reviewed. Currently, no antidepressants, 
including venlafaxine, are approved for the treatment of chronic pain 
syndromes. Addnl. randomized, controlled trials are necessary to fully 
elucidate the role of venlafaxine in the treatment of chronic pain. 



REFERENCE COUNT: 



59 THERE ARE 59 CITED REFERENCES AVAILABLE FOR THIS 
RECORD. ALL CITATIONS AVAILABLE IN THE RE FORMAT 



L34 ANSWER 4 OF 4 HCAPLUS COPYRIGHT 2005 ACS on STN 



:^:r:^!::::^:w^^^^::::^X:^x^ 

Full 




Sot 




Text 


iiii 




^^^^ 



ACCESSION NUMBER: 
DOCUMENT NUMBER: 
TITLE: 
AUTHOR (S) : 
CORPORATE SOURCE: 

SOURCE : 



1998 : 469364 HCAPLUS 
129:239318 

Potential applications of venlafaxine 
Nutt, D.; Johnson, F. Neil 

School of Medical Sciences/ University of Bristol, 
Bristol, BS8 ITD, UK 

Reviews in Conten^orary Pharmacotherapy (1998), 9(5), 



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Page 19 of 24 



321-331 

CODEN: RCPHFW; ISSN: 0954-8602 
PUBLISHER: Marius Press 

DOCUMENT TYPE: Journal; General Review 

LANGUAGE: English 

AB A review with 95 refs. The action of venlafaxine on at least two 

neurotransmitter systems suggests that this agent may have potential 
applications in a variety of conditions in addn. to the treatment of 
depression. Evidence on the point is relatively scanty at the present 
time, but such information as is available suggests that venlafaxine may 
have a future role in the management of several psychiatric conditions. 
These include: obsessive-compulsive disorder; panic disorder; attention 
deficit hyper-activity disorder (in children and in adults); borderline 
personality disorder; chronic fatigue syndrome; and possibly loss of 
libido and/or erectile dysfunction. There are also suggestions of 
therapeutic benefit arising from venlafaxine treatment of phobic 
conditions, specifically agoraphobia and social phobia. Recent work 
indicates that venlafaxine may reduce anxiety concomitant with 
depressive symptoms as well as anxiety occurring in the absence of 
depression, and that it may be rather more effective in doing so than is 
the case for several comparator agents. Venlafaxine appears to be 
effective in treating certain forms of pain; this is particularly evident 
against some types of headache, and there are indications of efficacy also 
against postherpetic neuralgia, chronic radicular back pain, and 
fibromyalgia. While venlafaxine has been found to show some degree of 
efficacy against Raynaud's phenomenon, it is unlikely to be better than 
selective serotonin reuptake inhibitors in the treatment of this 
condition. Further studies of venlafaxine are likely to reveal a wider 
spectrum of potential applications for this agent. 

REFERENCE COUNT: '95 THERE ARE 95 CITED REFERENCES AVAILABLE FOR THIS 

RECORD. ALL CITATIONS AVAILMLE IN THE RE FORMAT 



=> d his 

(FILE 'HOME' ENTERED AT 12:05:34 ON 22 NOV 2005) 
FILE 'REGISTRY' ENTERED AT 12:09:17 ON 22 NOV 2005 

FILE 'MEDLINE, BIOSIS, EMBASE, HCAPLUS ' ENTERED AT 12:09:40 ON 22 NOV 2005 



LI OS VENLAFAXINE () POST () TRAUMATIC () STRESS 

L2 7 S VENLAFAXINE? () DERIVATIVE? 

L3 IS VENLAFAXINE () ANALOG? 

L4 0 S L2 AND REVIEW/DT 

L5 8967 S VENLAFAXINE? 

L6 626478 S SENILE () DEMENTIA? OR PARKINSON? () DISEASE? OR EPILEPSY? OR 

L7 12 S L6 0 L5 

L8 1 S L7 AND REVIEW/DT 

L9 187794 S SCHIZOPHRENIA OR BORDERLINE () PERSONALITY () DISORDER? 

LIO 1 S L9 0 L5 

Lll 0 S LIO AND REVIEW/DT 

L12 4026 S COCAINE () ADDICTION OR ALCOHOL {) ADDICTION? 

L13 0 S L12 0 L5 

L14 9 S L12 AND L5 

L15 0 S L14 AND REVIEW/DT 

L16 16028 S BULIMIA () NERVOSA? OR GILLES? () TOURETTE () SYNDROME OR VAS 

L17 0 S L16 0 L5 

L18 66 S L16 AND L5 

LI 9 4 S L18 AND REVIEW/DT 

L20 36 S L5 AND URINARY () INCONTINENCE? 



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L21 


1 


S 


L20 AND REVIEW/DT 


L22 


3134 


S 


CENTRAL 0 NERVOUS {) SYSTEM? () DISORDER? 


L23 


18 


S 


L22 AND URINARY () INCONTINENCE? 


L24 


1 


S 


L23 AND REVIEW/DT 


L25 


37137 


s 


CHRONIC 0 OBSTRUCTIVE () PULMONARY () DISEASE? 


L26 


1 


s 


L25 AND L5 


L27 


0 


s 


L26 AND REVIEW/DT 


L28 


780 


s 


L5 AND PAIN? 


L29 


3 


s 


L5 ( ) PAIN 


L30 


1 


s 


L29 AND REVIEW/DT 


L31 


3164 


s 


POSTHERPETIC () NEURALGIA? 


L32 


0 


s 


L31 0 L5 


L33 


43 


s 


L31 AND L5 


L34 


4 


s 


L33 AND REVIEW/DT 



=> s sexual () dysfunction and IS 

L35 633 SEXUAL (W) DYSFUNCTION AND L5 

=> s 135 and review /dt 

L36 23 L35 AND REVIEW/DT 

=> is se:scual {) dysfunction? 

L37 17772 SEXUAL (W) DYSFUNCTION? 

=> s 15 {) 137 

L38 1 L5 (W) L37 

=> S5 I3S and rev.iev?/dt 

L39 0 L38 AND REVIEW/DT 

=> d 136; ibib abs, i'"4 



ANSWER 




MEDLINE on STN 



ACCESSION NUMBER: 
DOCUMENT NUMBER: 
TITLE: 



AB 



2004248907 MEDLINE 
PubMed ID: 15147109 

Tolerability issues during long-term treatment with 
antidepressants . 
Cassano Paolo; Fava Maurizio 

Depression Clinical and Research Program, Massachusetts 
.General Hospital, Boston, Massachusetts 02114, USA. . 
Pcassanofipartners . org 

Annals of clinical psychiatry : official journal of the 
American Academy of Clinical Psychiatrists, (2004 Jan-Mar) 
16 (1) 15-25. Ref: 111 

Journal code: 8911021. ISSN: 1040-1237. 
United States 

Journal; Article; (JOURNAL ARTICLE) 
General Review; (REVIEW) 

English 

Priority Journals 
200408 

Entered STN: 20040520 
Last Updated on STN: 20040811 
Entered Medline: 20040810 
Depressive disorders are highly prevalent in the general population. 
Long-term treatment with antidepressants consolidates the improvement 
obtained during the acute phase of the treatment and prevents relapses and 
recurrences of the disorder. On the other hand, there is growing evidence 



AUTHOR : 

CORPORATE SOURCE 



SOURCE : 



PUB. COUNTRY: 
DOCUMENT TYPE 

LANGUAGE : 
FILE SEGMENT: 
ENTRY MONTH: 
ENTRY DATE: 



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Page 21 of 24 



that antidepressant side effects may limit patients* quality of life and 
social functioning, as well as affect patients* health and treatment 
adherence. Most studies concerning antidepressant treatment have focused 
on short-term tolerability, ignoring both early-onset persistent side 
effects and late-onset side effects that are reported during long-term 
treatment. Nevertheless, these long-term treatment side effects are 
likely to have a dramatic impact on patient outcome and treatment 
adherence. Common long-term side effects of antidepressants are weight 
gain, sexual dysfunction, sleep disturbances, fatigue, apathy, and 
cognitive impairment (e.g., working memory dysfunction). Usual strategies 
for the management of these long-term side effects are: changing drug 
daily schedule, various augmentation therapies, antidepressant switches, 
drug-holidays, and dose tapering, with the latter two strategies being 
strongly discouraged on the basis of concerns that patients* depressive 
episodes may return. Selective serotonin reuptake inhibitors (SSRIs) and 
atypical antidepressants (e.g., venlafaxine, bupropion, and nefazodone) 
show a relatively favorable short-term as well as long-term tolerability 
compared with older drugs (e.g., tricyclics and monoamine oxidase 
inhibitors) . Therefore, clinicians are likely to prefer them in usual 
practice, especially among patients requiring maintenance treatment. The 
present review focuses on management of long-term side effects. 



L36 ANSWER 2 OF 23 



MEDLINE on STN 



ACCESSION NUMBER 
DOCUMENT NUMBER: 
TITLE: 
COMMENT : 



AUTHOR: 

CORPORATE 
SOURCE : 



SOURCE : 



2004050011 MEDLINE 
PubMed ID: 14750401 

Diabetic neuropathy: an intensive review. 
Comment in: Am J Health Syst Pharm. 2004 Jul 
15; 61 (14) : 1446-7; author reply 1447. PubMed ID: 15332691 
Duby Jeremiah John; Campbell R Keith; Setter Stephen M; 
White John Raymond; Rasmussen Kristin A 
University of Arizona, Tucson, AZ, USA. 
American journal of health-system pharmacy : AJHP : 
official journal of the American Society of Health-System 
Pharmacists, (2004 Jan 15) 61 (2) 160-73; quiz 175-6. Ref: 
90 

Journal code: 9503023. ISSN: 1079-2082. 
United States 

Journal; Article; (JOURNAL ARTICLE) 
General Review; (REVIEW) 
English 

Priority Journals 

200404 

Entered STN: 20040131 
Last Updated on STN: 20040414 
Entered Medline: 20040413 
PURPOSE: The epidemiology, classification, pathology, and treatment of 
diabetic neuropathy are reviewed. SUMMARY: Diabetic peripheral neuropathy 
is a common complication of diabetes that can cause significant morbidity 
and mortality. Some 30% of hospitalized and 20% of community-dwelling 
diabetes patients have peripheral neuropathy; the annual incidence rate is 
approximately 2%. The primary risk factor is hyperglycemia. Sensorimotor 
neuropathy is marked by pain, paresthesia, and sensory loss. Cardiac 
autonomic neuropathy (CAN) may contribute to myocardial infarction, 
malignant arrhythmia, and sudden death. Gastroparesis is the most 
debilitating complication of gastrointestinal autonomic neuropathy. 
Genitourinary autonomic neuropathy can cause sexual dysfunction and 
neurogenic bladder. The pathology of diabetic neuropathy involves 
oxidative stress, advanced glycation end products, polyol pathway flux. 



PUB . COUNTRY : 
DOCUMENT TYPE 

LANGUAGE : 
FILE SEGMENT: 
ENTRY MONTH: 
ENTRY DATE: 



AB 



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Page 22 of 24 



and protein kinase C activation; all contribute to microvascular disease 
and nerve dysfunction. For symptom management current evidence from 
clinical trials supports the use of desipramine, amitriptyline, capsaicin, 
tramadol, gabapentin, bupropion, and venlafaxine as preferred 
medications. Citalopram, nonsteroidal antiinflammatory drugs, and opioid 
analgesics may be used as adjuvant agents. Lamotrigine, oxcarbazepine, 
paroxetine, levodopa, and alpha-lipoic acid are alternative 
considerations. Evidence supporting the use of zonisamide, fluoxetine, 
mexiletine, dextromethorphan, and phenytoin is considered equivocal. 
Complementary therapies have also shown efficacy. The symptoms of CAN may 
be ameliorated with fludrocortisone, clonidine, midodrine, 
dihydroergotamine or caffeine, octreotide, and beta-blockers. 
Gastroparesis may be treated with metoclopramide or erythromycin. The 
most promising disease-modifying therapy is ruboxistaurin, which is in 
Phase III trials. Glycemic control remains the foundation of prevention 
and the prerequisite of adequate treatment. CONCLUSION: Diabetic 
neuropathy is a many-faceted complication of diabetes that can be managed 
symptomatically with an array of drugs. 



L36 ANSWER 3 OF 23 



MEDLINE on STN 



ACCESSION NUMBER 
DOCUMENT NUMBER: 
TITLE: 



2003152679 MEDLINE 
PubMed ID: 12667885 

Side effects of androgen deprivation therapy: monitoring 
and minimizing toxicity. 
Higano Celestia S 

Department of Urology, University of Washington School of 
Medicine, University of Washington, Seattle Cancer Care 
Alliance, Seattle, Washington 98109, USA. . 
thiqanoQuwashinqton . edu 

Urology, (2003 Feb) 61 (2 Suppl 1) 32-8. Ref: 43 
Journal code: 0366151. ISSN: 1527-9995. 
United States 

Journal; Article; (JOURNAL ARTICLE) 
General Review; (REVIEW) 

(REVIEW, TUTORIAL) 
English 

Priority Journals 
200307 

Entered STN: 20030402 
Last Updated on STN: 20030702 
Entered Medline: 20030701 
The current trends in favor of androgen deprivation therapy (ADT) for 
nonmetastatic prostate cancer at the stage of biochemical recurrence or 
increasing prostate-specific antigen (PSA) raises the issue of exposing 
otherwise asymptomatic patients to potential side effects over the longer 
term. Some of these side effects can have deleterious effects on quality 
of life, and others may contribute to increased risks for serious health 
concerns associated with aging. Sexual side effects are the most 
well-recognized adverse effects from ADT and include loss of libido, 
erectile dysfunction (ED), and hot flashes. Loss of libido is distressing 
to many men, and they may not pursue treatments for ED. However, for 
those who do maintain sexual interest, various remedies are available. 
The incidence of hot flashes, which may not abate over the course of ADT, 
is close to 80%. Estrogens, progestin megestrol acetate, 
medroxyprogesterone acetate, venlafaxine, and cyproterone acetate have 
been shown to alleviate hot flashes and associated symptoms. Physiologic 
effects, including gynecomastia, changes in body composition (weight gain, 
reduced muscle mass, increase in body fat) , and changes in lipids, are 



AUTHOR: 

CORPORATE SOURCE 



SOURCE : 

PUB. COUNTRY: 
DOCUMENT TYPE 



LANGUAGE : 
FILE SEGMENT 
ENTRY MONTH: 
ENTRY DATE: 



AB 



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Page 23 of 24 



less commonly recognized as side effects of ADT. These may lead to an 
exacerbation of potentially more serious conditions, such as hypertension, 
diabetes, and coronary artery disease. Loss of bone mineral density, 
anemia, and hair changes also may occur. Additionally, both the diagnosis 
of prostate cancer and the hormonal therapy can cause psychological 
distress. These side effects need more systematic study in clinical 
trials. Physicians should be aware of far-reaching consequences of ADT 
and should incorporate strategies for preventing and managing toxicities 
into routine practice. 



L36 ANSWER 4 OF 23 



MEDLINE on STN 



AUTHOR : 

CORPORATE SOURCE: 
SOURCE : 



PUB. COUNTRY: 
DOCUMENT TYPE 



LANGUAGE : 
FILE SEGMENT 
ENTRY MONTH: 
ENTRY DATE: 



:1874 
:1049 

Spartanburg, 
547-54. 



ACCESSION NUMBER: 2003076790 MEDLINE 
DOCUMENT NUMBER: PubMed ID: 12588077 

TITLE: Antidepressants: update on new agents and indications. 

COMMENT: Comment in: Am Fam Physician. 2004 Jun 1; 69 ( 11) : 2528; 

author reply 2528. PubMed ID: 15202688 
Erratum in: Am Fam Physician. 2003 May 1;67(9) 
Erratum in: Am Fam Physician. 2004 Mar 1;69(5) 
Abies Adrienne Z; Baughman Otis L 3rd 
Spartanburg Family Medicine Residency Program, 
South Carolina 29303, USA. . aablestgsrhs . com 
American family physician, (2003 Feb 1) 67 (3) 
Ref: 45 

Journal code: 1272646. ISSN: 0002-838X. 
United States 

Journal; Article; (JOURNAL ARTICLE) 
General Review; (REVIEW) 
(REVIEW, TUTORIAL) 

English 

Abridged Index Medicus Journals; Priority Journals 
200303 

Entered STN: 20030218 
Last Updated on STN: 20030313 
Entered Medline: 20030312 
A number of antidepressants have emerged in the U.S. market in the past 
two decades. Selective serotonin reuptake inhibitors have become the 
drugs of choice in the treatment of depression, and they are also 
effective in the treatment of obsessive-compulsive disorder, panic 
disorder, and social phobia. New indications for selective serotonin 
reuptake inhibitors include post-traumatic stress disorder, premenstrual 
dysphoric disorder, and generalized anxiety disorder. Extended-release 
venlafaxine has recently been approved by the U.S. Food and Drug 
Administration for the treatment of generalized anxiety disorder. 
Mirtazapine, which is unrelated to the selective serotonin reuptake 
inhibitors, is unique in its action — stimulating the release of 
norepinephrine and serotonin. The choice of antidepressant drug depends 
on the agent's pharmacologic profile, secondary actions, and tolerability . 
Sexual dysfunction related to the use of antidepressants may be 
addressed by reducing the dosage, switching to another agent, or adding 
another drug to overcome the sexual side effects. Augmentation with 
lithium or triiodothyronine may be useful in patients who are partially or 
totally resistant to antidepressant treatment. Finally, tapering 
antidepressant medication may help to avoid discontinuation syndrome or 
antidepressant withdrawal. 



AB 



=> js 13 () cognition? 

L40 2 L5 (W) COGNITION? 



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=> .<s .1.40 and revicsw/dt 

L41 0 L40 AND REVIEW/DT 

=> 



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=> s venlaf axii^e () derivative? 

LI 7 VENIiAFAXINE (W) DERIVATIVE? 

=> d llf ibib cEbs hitistr, 3-7 



ANSWER 3 OF 7 HCAPLUS COPYRIGHT 2005 ACS on STN 




ACCESSION NUMBER: 
DOCUMENT NUMBER: 
TITLE: 

INVENTOR (S) : 
PATENT ASSIGNEE (S): 
SOURCE : 

DOCUMENT TYPE: 
LANGUAGE : 

FAMILY ACC. NUM. COUNT: 
PATENT INFORMATION: 



2004:740168 HCAPLUS 
141:265967 

Silicon derivatives of venlafaxine for the treatment 

or prevention of psoriasis or panic disorder 

Showell, Graham Andrew 

Amedis Pharmaceuticals Ltd., UK 

PCT Int. Appl., 15 pp. 

CODEN: PIXXD2 

Patent 

English 

1 



PATENT NO. 



KIND DATE 



APPLICATION NO. 



DATE 



:004075902 




Al 




20040910 




WO 2004- 


GB662 




20040219 


W: 


AE, 


AE, 


AG, 


AL, 


AL, 


AM, 


AM, 


AM, 


AT, 


AT, 


AU, 


AZ, 


AZ, 


BA, 


BB, 


BG, 




BG, 


BR, 


BR, 


BW, 


BY, 


BY, 


BZ, 


BZ, 


CA, 


CH, 


CN, 


CN, 


CO, 


CO, 


CR, 


CR, 




CU, 


CU, 


CZ, 


CZ, 


DE, 


DE, 


DK, 


DK, 


DM, 


DZ, 


EC, 


EC, 


EE, 


EE, 


EG, 


ES, 




ES, 


FI, 


FI, 


GB, 


GD, 


GE, 


GE, 


GH, 


GM, 


HR, 


HR, 


HU, 


HU, 


ID, 


IL, 


IN, 




IS, 


JP, 


JP/ 


KE, 


KE, 


KG, 


KG, 


KP, 


KP, 


KP, 


KR, 


KR, 


KZ, 


KZ, 


KZ, 


LC, 




LK, 


LR, 


LS, 


LS, 


LT, 


LU, 


LV, 


MA, 


MD, 


MD, 


MG, 


MK, 


MN, 


MW, 


MX, 


MX, 




MZ, 


MZ, 


NA, 


NI 


























RW: 


BW, 


GH, 


GM, 


KE, 


LS, 


MW, 


MZ, 


SD, 


SL, 


SZ, 


TZ, 


UG, 


ZM, 


ZW, 


AT, 


BE, 




BG, 


CH, 


CY, 


CZ, 


DE, 


DK, 


EE, 


ES, 


FI, 


FR, 


GB, 


GR, 


HU, 


IE, 


IT, 


LU, 




MC, 


NL, 


PT, 


RO, 


SE, 


SI, 


SK, 


TR, 


BF, 


BJ, 


CF, 


CG, 


CI, 


CM, 


GA, 


GN, 




GQ, 


GW, 


ML, 


MR, 


NE, 


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TD, 


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GA, 


GN, 




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GW, 


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TD, 


TG 


















APPLN. 


INFO 














GB 2003- 


4646 






A 20030228 




















GB 2003- 


4647 






A 20030228 



OTHER SOURCE(S): MARPAT 141:265967 

AB A silicon deriv. of venlafaxine such as 1- [2-dimethylamino-l- ( 4- 

methoxyphenyl) ethyl] -1-silacyclohexan-l-ol or a salt thereof or a prodrug 
form that is hydrolyzable for the manuf . of a medicament for the treatment 
or prevention of psoriasis or panic disorder is disclosed. 

REFERENCE COUNT: 5 THERE ARE 5 CITED REFERENCES AVAILABLE FOR THIS 

RECORD. ALL CITATIONS AVAILABLE IN THE RE FORMAT 



LI 



ANSWER 4 OF 7 HCAPLUS COPYRIGHT 2005 ACS on STN 







Text 





ACCESSION NUMBER: 
DOCUMENT NUMBER: 
TITLE : 

INVENTOR (S) : 
PATENT ASSIGNEE (S) : 
SOURCE : 

DOCUMENT TYPE: 
LANGUAGE : 

FAMILY ACC. NUM. COUNT: 



2000:725583 HCAPLUS 
133:296268 

Preparation of derivatives of venlafaxine and their 

inhibition of neuronal monoamine reuptake 

Jerussi, Thomas P.; Senanayake, Chrisantha H. 

Sepracor Inc., USA 

PCT Int. Appl., 40 pp. 

CODEN: PIXXD2 

Patent 

English 

1 



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Pages of 6 



PATENT INFORMATION: 



PATENT NO. 



KIND DATE 



APPLICATION NO. 



DATE 



WO 


2000059851 




Al 




20001012 




WO 2000- 


US8705 




20000331 




W: 


AE, 


AG, 


AL, 


AM, 


AT, 


AU, 


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ID, 


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ES, 


FI, 


FR, 


GB, 


GR, 


IE, 


IT, 


LU, MC, 


NL, PT, 


SE, 


BF, BJ, CF, 






CG, 


CI, 


CM, 


GA, 


GN, 


GW, 


ML, 


MR, 


NE, SN, 


TD, TG 






CA 


2368083 






AA 




20001012 




CA 2000- 


2368083 




20000331 


EP 


1165487 






Al 




20020102 




EP 2000- 


920026 




20000331 




R: 


AT, 
IE, 


BE, 
SI, 


CH, 
LT, 


DE, 
LV, 


DK, 
FI, 


ES, 
RO 


FR, 


GB, 


GR, IT, 


LI, LU, 


NL, 


SE, MC, PT, 


JP 


2003521470 




T2 




20030715 




JP 2000- 


609367 




20000331 


NZ 


514612 






A 




20040130 




NZ 2000- 


514612 




20000331 


EP 


1466889 






Al 




20041013 




EP 2004- 


10248 




20000331 




R: 


AT, 


BE, 


CH, 


DE, 


DK, 


ES, 


FR, 


GB, 


GR, IT, 


LI, LU, 


NL, 


SE, MC, PT, 






IE, 


SI, 


LT, 


LV, 


FI, 


RO, 


MK, 


CY, 


AL 








AU 


782092 






B2 




20050630 




AU 2000- 


40627 




20000331 


NO 


2001004816 




A 




20011204 




NO 2001- 


4816 




20011003 


US 


2004106576 




Al 




20040603 




US 2003- 


720134 




20031125 


US 


2005197392 




Al 




20050908 




US 2005- 


91518 




20050329 


IITY APPLN. 


INFO. 














US 1999- 


127938P 




P 19990406 






















US 1999- 


167906P 




P 19991130 






















US 2000- 


527442 




A3 20000317 






















EP 2000- 


920026 




A3 20000331 






















WO 2000- 


US8705 




W 20000331 






















US 2003- 


720134 




A3 20031125 



AB Prepn. of derivs. of venlafaxine, e.g., 0-desmethylvenlaf laxine, is 

described. Also disclosed are methods of treating and preventing diseases 
and disorders including, but not limited to, affective disorders such as 
depression, bipolar and manic disorders, attention deficit disorder, 
attention deficit disorder with hyperactivity, Parkinson's disease, 
epilepsy, cerebral function disorders, obesity and wt. gain, incontinence, 
dementia and related disorders. 



REFERENCE 


COUNT: 


5 


THERE ARE 5 CITED REFERENCES AVAILABLE 
RECORD. ALL CITATIONS AVAILABLE IN THE 


FOR THIS 
RE FORMAT 


LI ANSWER 5 OF 7 


HCAPLUS 


COPYRIGHT 2005 ACS on STN 




r^"' Tutr 

Text 










ACCESSION 


NUMBER: 


2000 


: 38 4124 HCAPLUS 





DOCUMENT NUMBER: 
TITLE: 

INVENTOR (S) : 
PATENT ASSIGNEE (S) : 
SOURCE : 

DOCUMENT TYPE: 
LANGUAGE : 

FAMILY ACC. NUM. COUNT: 
PATENT INFORMATION: 



133:17270 

Preparation of {-) -venlafaxine and derivatives as 

neuronal monoamine reuptake inhibitors. 

Jerussi, Thomas P.; Senanayake, Chrisantha H. 

Sepracor Inc., USA 

PCT Int. Appl., 45 pp. 

CODEN: PIXXD2 

Patent 

English 

1 



PATENT NO. 



KIND DATE 



APPLICATION NO. 



DATE 



http://stnwebxas.org/cgi-bin/sdcgi?SID=61366-2007567098-200&APP=stnweb& 



11/22/05 



Page 4 of 6 



WO 


2000032556 




Al 




20000608 




WO 1999- 


US28303 




19991201 




W: AE, 


AL, 


AM, 


AT, 


AU, 


AZ, 


BA, 


BB, 


BG, BR, 


BY, 


CA, 


CH, 


CN, CR, CU, 




CZ, 


DE, 


DK, 


EE, 


ES, 


FI, 


GB, 


GD, 


GE, GH, 


GM, 


HR, 


HU, 


ID, IL, IN, 




IS, 


JP, 


KE, 


KG, 


KP, 


KR, 


KZ, 


LC, 


LK, LR, 


LS, 


LT, 


LU, 


LV, MA, MD, 




MG, 


MK, 


MN, 


MW, 


MX, 


NO, 


NZ, 


PL, 


PT, RO, 


RU, 


SD, 


SE, 


SG, SI, SK, 




SL, 


TJ, 


TM, 


TR, 


TT, 


UA, 


UG, 


UZ, 


VN, YU, 


ZA, 


ZW, 


AM, 


AZ, BY, KG, 




KZ, 


MD, 


RU, 


TJ, 


TM 




















RW: GH, 


GM, 


KE, 


LS, 


MW, 


SD, 


SL, 


SZ, 


TZ, UG, 


zw. 


AT, 


BE, 


CH, CY, DE, 




DK, 


ES, 


FI, 


FR, 


GB, 


GR, 


IE, 


IT, 


LU, MC, 


NL, 


PT, 


SE, 


BF, BJ, CF, 




CG, 


CI, 


CM, 


GA, 


GN, 


GW, 


ML, 


MR, 


NE, SN, 


TD, 


TG 






us 


6342533 






Bl 




20020129 




US 1999- 


450690 




19991130 


CA 


2352324 






AA 




20000608 




CA 1999- 


2352324 




19991201 


EP 


1135359 






Al 




20010926 




EP 1999- 


968056 




19991201 




R: AT, 


BE, 


CH, 


DE, 


DK, 


ES, 


FR, 


GB, 


GR, IT, 


LI, 


LU, 


NL, 


SE, MC, PT, 




IE, 


SI, 


LT, 


LV, 


FI, 


RO 
















JP 


2003524613 




T2 




20030819 




JP 2000- 


585198 




19991201 


AU 


774408 






B2 




20040624 




AU 2000- 


24749 




19991201 


US 


2002086904 




Al 




20020704 




US 2001- 


14592 




20011214 


US 


6441048 






B2 




20020827 














US 


2003018083 




Al 




20030123 




US 2002- 


222815 




20020819 


us 


6911479 






B2 




20050628 














us 


2004180952 




Al 




20040916 




US 2004- 


806423 




20040323 



PRIORITY APPLN. INFO.: US 1998-11Q438P P 19981201 

US 1999-450690 A 19991130 

WO 1999-US28303 W 19991201 

US 2001-14592 A3 20011214 

US 2002-222815 A3 20020819 

AB A pharmaceutical compn. comprising ( - ) -venlaf axine deriv. 
substantially free of (+) -stereoisomer is claimed. Thus, 
(?) -venlaf axine in THF was added to a mixt. prepd. from Ph2PH and BuLi 
in THF at 0? followed by stirring and overnight reflux to give 
73.8% (?) -0-desmethylvenlaf axine, which was resolved using 
di-p-toluoyl-L-tartaric acid to give (-) -0-desmethylvenlaf axine . Drug 
formulations contg. the latter are given. 
REFERENCE COUNT: 2 THERE ARE 2 CITED REFERENCES AVAILABLE FOR THIS 

RECORD. ALL CITATIONS AVAILABLE IN THE RE FORMAT 



LI ANSWER 6 OF 7 HCAPLUS COPYRIGHT 2005 ACS on STN 









Text 







ACCESSION NUMBER: 
DOCUMENT NUMBER: 
TITLE: 

INVENTOR (S) : 
PATENT ASSIGNEE (S): 
SOURCE : 

DOCUMENT TYPE: 
LANGUAGE : 

FAMILY ACC. NUM. COUNT: 
PATENT INFORMATION: 



2000: 384122 HCAPLUS 
133:30575 

Preparation of derivatives of (+) -venlaf axine as 

inhibitors of neuronal monoamine reuptake. 

Jerussi, Thomas P.; Senannayake, Chrisantha H. 

Sepracor Inc., USA 

PCT Int. Appl., 47 pp. 

CODEN: PIXXD2 

Patent 

English 

1 



PATENT NO. KIND DATE 



WO 2000032555 Al 20000608 

W: AE, AL, AM, AT, AU, AZ, BA, 

CZ, DE, DK, EE, ES, FI, GB, 

IS, JP, KE, KG, KP, KR, KZ, 



APPLICATION NO. DATE 



WO 1999-US28306 19991201 

BB, BG, BR, BY, CA, CH, CN, CR, CU, 

GD, GE, GH, GM, HR, HU, ID, IL, IN, 

LC, LK, LR, LS, LT, LU, LV, MA, MD, 



http://stnweb.cas.org/cgi-bin/sdcgi?SID=61366-2007567098-200&APP=stnweb& 



11/22/05 



Page 5 of 6 



MG, MK, MN, MW, MX, NO, NZ, PL, PT, RO, RU, SD, SE, SG, SI, SK, 

SL, TJ, TM, TR, TT, UA, UG, UZ, VN, YU, ZA, ZW, AM, AZ, BY, KG, 

KZ, MD, RU, TJ, TM 
RW: GH, GM, KE, LS, MW, SD, SL, SZ, TZ, UG, ZW, AT, BE, CH, CY, DE, 

DK, ES, FI, FR, GB, GR, IE, IT, LU, MC, NL, PT, SE, BF, BJ, CF, 

CG, CI, CM, GA, GN, GW, ML, MR, NE, SN, TD, TG 
US 619782S Bl 20010306 US 1999-450691 19991130 

CA 2352321 AA 20000608 CA 1999-2352321 19991201 

EP 1135358 Al 20010926 EP 1999-965065 19991201 

R: AT, BE, CH, DE, DK, ES, FR, GB, GR, IT, LI, LU, NL, SE, MC, PT, 

IE, FI 

JP 2003501344 T2 20030114 JP 2000-585197 19991201 

PRIORITY APPLN. INFO. : US 1998-110436P P 19981201 

US 1999-450691 A 19991130 

WO 1999-US28306 W 19991201 

AB A method of treating an affective disorder comprises administration of a 

(+) -venlafaxine deriv. substantially free of the (-) -enantiomer . 

Thus, (?) -venlafaxine (prepn. given) was added to a 0? mixt. of 

Ph2PH and BuLi followed by stirring and reflux overnight to give 73.8% 

(?) -O-desmethyl venlafaxine, which was resolved to give 

(+) -0-desmethyl venlafaxine . Drug formulations contg. the latter are 

given. 

REFERENCE COUNT: 10 THERE ARE 10 CITED REFERENCES AVAILABLE FOR THIS 

RECORD. ALL CITATIONS AVAILABLE IN THE RE FORMAT 



ANSWER 7 OF 7 HCAPLUS COPYRIGHT 2005 ACS on STN 




ACCESSION NUMBER: 
DOCUMENT NUMBER: 
TITLE: 

INVENTOR (S) : 

PATENT ASSIGNEE (S) : 
SOURCE : 

DOCUMENT TYPE: 
lANGUAGE : 

FAMILY ACC. NUM. COUNT: 
PATENT INFORMATION: 



1998 : 323132 HCAPLUS 
129:23447 

A method for treating tension-type headache 

Olesen, Jes; Bendtsen, Lars; Jensen, Rigmor; Madsen, 

Ulf 

Den. 

PCT Int. Appl., 142 pp. 

CODEN: PIXXD2 

Patent 

English 

1 



PATENT NO. KIND DATE 



WO 


9819674 






A2 




19980514 


wo 


9819674 






A3 




19980716 




W: 


AL, 


AM, 


AT, 


AT, 


AU, 


AZ, BA, 






CZ, 


DE, 


DE, 


DK, 


DK, 


EE, ES, 






JP, 


KE, 


KG, 


KP, 


KR, 


KZ, LC, 






MN, 


MW, 


MX, 


NO, 


NZ, 


PL, PT, 






TJ, 


TM, 


TR, 


TT, 


UA, 


UG, US, 






MD, 


RU, 


TJ, 


TM 








RW: 


GH, 


KE, 


LS, 


MW, 


SD, 


SZ, UG, 






GB, 


GR, 


IE, 


IT, 


LU, 


MC, NL, 






GN, 


ML, 


MR, 


NE, 


SN, 


TD, TG 


CA 


2270531 






AA 




19980514 


AU 


9748632 






Al 




19980529 


AU 


734490 






B2 




20010614 


EP 


1011656 






A2 




20000628 




R: 


AT, 


BE, 


CH, 


DE, 


DK, 


ES, FR, 






IE, 


SI, 


LT, 


LV, 


FI, 


RO 



APPLICATION NO. DATE 



WO 1997-DK502 19971104 



BB, 


BG, 


BR, 


BY, 


CA, 


CH, 


CN, 


CU, CZ, 


FI, 


FI, 


GB, 


GE, 


GH, 


HU, 


ID, 


IL, IS, 


LK, 


LR, 


LS, 


LT, 


LU, 


LV, 


MD, 


MG, MK, 


RO, 


RU, 


SD, 


SE, 


SG, 


SI, 


SK, 


SK, SL, 


UZ, 


VN, 


YU, 


ZW, 


AM, 


AZ, 


BY, 


KG, KZ, 


ZW, 


AT, 


BE, 


CH, 


DE, 


DK, 


ES, 


FI, FR, 


PT, 


SE, 


BF, 


BJ, 


CF, 


CG, 


CI, 


CM, GA, 




CA 1997- 


2270531 




19971104 




AU 1997- 


48632 




19971104 




EP 1997- 


911150 




19971104 


GB, 


GR, 


IT, 


LI, 


LU, 


NL, 


SE, 


MC, PT, 



http://stnweb.cas.org/cgi-bin/sdcgi?SID=61366-2007567098-200&APP=stnweb& 



11/22/05 



Page 6 of 6 



£P 


1132082 


Al 


20010912 


EP 


2000- 


204625 




19971104 




R: AT, BE, CH, 


DE, 


DK, ES, FR, 


GB, GR, IT, 


LI, LU, 


NL, SE 


1, MC, PT 




IE, FI 
















US 


6284794 


Bl 


20010904 


US 


1999- 


304115 




19990504 


AU 


771266 


B2 


20040318 


AU 


2001- 


57775 




20010802 


US 


2002072543 


Al 


20020613 


US 


2001- 


941855 




20010830 


US 


6649605 


B2 


20031118 












US 


2004097562 


Al 


20040520 


US 


2003- 


702497 




20031107 


PRIORITY 


' APPLN. INFO. : 






DK 


1996- 


1243 


A 


19961105 










US 


1996- 


30294P 


P 


19961105 










AU 


1997- 


48632 


A3 


19971104 










EP 


1997- 


911150 


A3 


19971104 










WO 


1997- 


DK502 


W 


19971104 










US 


1998- 


85413P 


P 


19980514 










US 


1999- 


304115 


A3 


19990504 










US 


2001- 


•941855 


A3 


20010830 



AB Tension-type headache is treated by interacting with neuronal transmission 
in relation to pain in connection with headache in a way which prevents or 
decreases sensitization of second order nociceptive neurons. In 
particular, treatment is performed by administration of an effective amt. 
of a substance which prevents or decreases central sensitization. 
Important examples of such substances are substances which interact with 
glutamate neurotransmission, such as glutamate receptor antagonists. 
Other examples are e.g. substances which interact with nitric oxide, such 
as nitric oxide synthase (NOS) inhibitors. According to a broader aspect 
of the invention, tension-type headache is treated by administration of 
substances which are effective in preventing or decreasing pain in 
connection with tension-type headache. An addnl . aspect of the invention 
relates to treatment of tension-type headache by administration of 
substances which substantially inhibit the activity of NOS. Evidence for 
central sensitization in chronic myofascial pain, as well as mechanisms of 
spontaneous tension-type headaches, are also described. Gabapentin and 
dextromethorphan had a prophylactic effect on chronic tension-type 
headaches . 



http://stnwebxas.org/cgi-bin/sdcgi?SID=61366-2007567098-200&APP=stnweb& 



11/22/05 



Page 1 of 1 



LIO ANSWER 15 OF 18 



HCAPLUS COPYRIGHT 2005 ACS on STN 




AUTHOR (S) : 
CORPORATE SOURCE: 



ACCESSION NUMBER: 
DOCUMENT NUMBER: 

TITLE: 



PUBLISHER: 
DOCUMENT TYPE: 
LANGUAGE : 



SOURCE : 



2004 : 583658 HCAPLUS 
141:184422 

Treatment of pain syndromes with venlafaxine 
Grothe, Dale R.; Scheckner/ Brian; Albano, Dominick 
Global Medical Communications, Neuroscience, Wyeth 
Pharmaceuticals, Collegeville, PA, USA 
Pharmacotherapy (2004) , 24 (5) , 621-629 
CODEN: PHPYDQ; ISSN: 0277-0008 
Pharmacotherapy Publications 
Journal; General Review 
English 



AB A review. Major depressive disorder (MDD) and anxiety disorders such as 
generalized anxiety disorder (GAD) are often accompanied by chronic 
painful symptoms. Examples of such symptoms are backache, headache, 
gastrointestinal pain, and joint pain. In addn., pain generally not 
assocd. with major depression or an anxiety disorder, such as peripheral 
neuropathic pain (e.g., diabetic neuropathy and postherpetic neuralgia), 
cancer pain, and fibromyalgia, can be challenging for primary care 
providers to treat. Antidepressants that block reuptake of both serotonin 
and norepinephrine, such as the tricyclic antidepressants (e.g., 
amitriptyline) , have been used to treat pain syndromes in patients with or 
without comorbid MDD or GAD. Venlafaxine, a serotonin and 
norepinephrine reuptake inhibitor, has been safe and effective in animal 
models, healthy human volunteers, and patients for treatment of various 
pain syndromes. The use of venlafaxine for treatment of pain assocd. 
with MDD or GAD, neuropathic pain, headache, fibromyalgia, and 
postmastectomy pain syndrome is reviewed. Currently, no antidepressants, 
including venlafaxine, are approved for the treatment of chronic 
pain syndromes. Addnl. randomized, controlled trials are necessary to 
fully elucidate the role of venlafaxine in the treatment of chronic pain. 

REFERENCE COUNT: 59 THERE ARE 59 CITED REFERENCES AVAILABLE FOR THIS ^ 



RECORD. ALL CITATIONS AVAILABLE IN THE RE FORMAT 



http://stoweb.cas.org/cgi-bin/sdcgi?SID=71038-1697741594-200&APP=stnweb& 



11/22/05 



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FILE COVERS 1907 - 22 Nov 2005 VOL 143 ISS 22 
FILE LAST UPDATED: 21 Nov 2005 (20051121/ED) 



New CAS Information Use Policies, enter HELP USAGETERMS for details. 

This file contains CAS Registry Numbers for easy and accurate 
substance identification. 



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109 
731132 
L4 38 



L3 

THU/RL 
L3/THU 

(L3 (L) THU/RL) 



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L4 



ANSWER 1 OF 38 HCAPLUS COPYRIGHT 2005 ACS on STN 







mm 




Text 






iiii 



ACCESSION NUMBER: 
TITLE: 

INVENTOR (S) : 
PATENT ASSIGNEE (S) 
SOURCE : 



DOCUMENT TYPE: 

LTU^GUAGE : 

FAMILY ACC. NUM. COUNT: 
PATENT INFORMATION: 



2005:1175135 HCAPLUS 

Modif ied-release compositions of at least one form of 
venlaf axine 

Seth, Pawan; Maes, Paul J. 

Biovail Laboratories, Inc., Barbados 

U.S. Pat. Appl. Publ., 36 pp., Cont . -in-part of U.S. 

Ser. No. 244,059. 

CODEN: USXXCO 

Patent 

English 

3 



PATENT NO. 


KIND 


DATE 


APPLICATION NO. 




DATE 


US 2005244498 


Al 


20051103 


US 2004-3028 




20041203 


US 2003059466 


Al 


20030327 


US 2001-953101 




20010914 


US 2003091634 


Al 


20030515 


US 2002-244059 




20020913 


PRIORITY APPLN. INFO.: 






US 2001-953101 


A2 


20010914 








US 2002-244059 


A2 


20020913 



AB The present invention relates to a modified release compn. of at least one 
form of venlafaxine, which is an enhanced absorption delayed 
controlled- release compn. for oral administration suitable for once daily 
dosing. The compn. comprises a core comprising at least one form of 
venlafaxine selected from the group consisting of venlafaxine, an active 
metabolite of venlafaxine, a pharmaceutically acceptable salt of 



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venlafaxine, a pharmaceutically acceptable salt of an active metabolite of 
venlafaxine, and combinations thereof^ and a pharmaceutically acceptable 
excipient. The compn. further comprises a modified release coating which 
substantially surrounds the core. The compns . of the invention provide 
enhanced absorption delayed controlled release of the at least one form of 
venlafaxine such that the combined geometric mean ratio of the compn. of 
the invention to the ref . product for the AUCO-t or the Cmax for 
venlafaxine and its active metabolite 0-desmethylvenlaf axine is greater 
than 2 after first administration of the compn. under fed or fasting 
conditions. Tablets contg. venlafaxine hydrochloride 169.71, lactose 
71.29, hydroxypropyl Me cellulose 40.00, polyvinylpyrrolidone 2.00 mg in 
the core and ethocel-100 12.650, Kollidon 90F 7.245, and stearic acid 
31.05 mg in the coating were prepd. The amt. of venlafaxine released 
after 8 h was 100% . 

IT 93413-62-8 / 0-Desmethylvenlaf axine 

RL: PAC (Pharmacological activity); THU (Therapeutic use); BIOL 
(Biological study); USES (Uses) 

(modified- release compns. of at least one form of venlafaxine) 

RN 93413-62-8 HCAPLUS 

CN Phenol, 4- [2- (dimethyl ami no) -1- (1-hydroxycyclohexyl) ethyl] - (9CI) (CA 
INDEX NAME) 




IT 448904-47-0 

RL: THU (Therapeutic use); BIOL' (Biological study); USES (Uses) 
(modified- release compns. of at least one form of venlafaxine) 
RN 448904-47-0 HCAPLUS 

CN Butanedioic acid, compd. with 4- [2- (dimethylamino) -1- (1- 

hydroxycyclohexyl) ethyl] phenol (1:1) (9CI) (CA INDEX NAME) 

CM 1 

CRN 93413-62-8 
CMF C16 H25 N 02 




CM 2 

CRN 110-15-6 
CMF C4 H6 04 



L4 ANSWER 2 OF 38 HCAPLUS COPYRIGHT 2005 ACS on STN 




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ACCESSION NUMBER: 
DOCUMENT NUMBER: 
TITLE: 

INVENTOR (S) : 
PATENT ASSIGNEE (S) 
SOURCE : 



DOCUMENT TYPE: 
LANGUAGE : 

F7\MILY ACC. NUM. COUNT: 
PATENT INFORMATION: 



2005: 1004355 HCAPLUS 
143:279430 

Use of D4 and 5-HT2a antagonists, inverse agonists or 
partial agonists 
Buntinx, Erik 
Belg. 

U.S. Pat. Appl. Publ., 126 pp., Cont . -in-part of U.S. 

Ser. No. 803,793. 

CODEN: USXXCO 

Patent 

English 

6 



PATENT NO. KIND DATE APPLICATION NO. DATE 



US 


2005203130 




Al 




20050915 




US 2004- 


984683 




20041109 


us 


2005119253 




Al 




20050602 




US 2003- 


725965 




20031202 


us 


2005119248 




Al 




20050602 




US 2004- 


752423 




20040106 


us 


2005119249 




Al 




20050602 




US 2004- 


803793 




20040318 


EP 


1541197 






Al 




20050615 




EP 2004- 


25035 




20041021 




R: AT, 


BE, 


CH, 


DE, 


DK, 


ES, 




GB, 


GR, IT, 


LI, LU, 


NL, 


SE, MC, PT, 




IE, 


SI, 


LT, 


LV, 


FI, 


RO, 


MK, 


CY, 


AL, TR, 


BG, CZ, 


EE, 


HU, PL, SK, HR 


WO 


2005053796 




Al 




20050616 




WO 2004- 


BE 172 




20041202 




W: AE, 


AG, 


AL, 


AM, 


AT, 


AU, 


AZ, 


BA, 


BB, BG, 


BR, BW, 


BY, 


BZ, CA, CH, 




CN, 


CO, 


CR, 


CU, 


CZ, 


DE, 


DK, 


DM, 


DZ, EC, 


EE, EG, 


ES, 


FI, GB, GD, 




GE, 


GH, 


GM, 


HR, 


HU, 


ID, 


IL, 


IN, 


IS, JP, 


KE, KG, 


KP, 


KR , KZ , LC , 




LK, 


LR, 


LS, 


LT, 


LU, 


LV, 


MA, 


MD, 


MG, MK, 


MN, MW, 


MX, 


MZ, NA, NI, 




NO, 


NZ, 


OM, 


PG, 


PH, 


PL, 


PT, 


RO, 


RU, SC, 


SD, SE, 


SG, 


SK, SL, SY, 




TJ, 


TM, 


TN, 


TR, 


TT, 


TZ, 


UA, 


UG, 


US, UZ, 


VC, VN, 


YU, 


ZA, ZM, ZW 




RW: BW, 


GH, 


GM, 


KE, 


LS, 


MW, 


MZ, 


NA, 


SD, SL, 


SZ, TZ, 


UG, 


ZM, ZW, AM, 




AZ, 


BY, 


KG, 


KZ, 


MD, 


RU, 


TJ, 


TM, 


AT, BE, 


BG, CH, 


CY, 


CZ, DE, DK, 




EE, 


ES, 


FI, 


FR, 


GB, 


GR, 


HU, 


IE, 


IS, IT, 


LT, LU, 


MC, 


NL, PL, PT, 




RO, 


SE, 


SI, 


SK, 


TR, 


BF, 


BJ, 


CF, 


CG, CI, 


CM, GA, 


GN, 


GQ, GW, ML, 




MR, 


NE, 


SN, 


TD, 


TG 
















PRIORITY 


' APPLN. 


INFO. 














US 2003- 


725965 




A2 20031202 




















EP 2004- 


447001 




A 20040105 




















US 2004- 


752423 




A2 20040106 




















US 2004- 


803793 




A2 20040318 




















EP 2004- 


25035 




A 20041021 




















CA 2003- 


2451798 




A 20031202 




















EP 2003- 


447279 




A 20031202 




















CA 2004- 


2461248 




A 20040318 




















EP 2004- 


447066 




A 20040318 




















JP 2004- 


349085 




A 20041104 




















US 2004- 


984683 




A 20041109 




















CA 2004- 


2487529 




A 20041115 



AB The present invention relates to the use of compds . and compns . of compds . 
having D4 and 5-HT2A antagonistic, partial agonistic or inverse agonistic 
activity for the treatment of the underlying dysregulation of the 
emotional functionality of mental disorders (i.e. affect 

instability-hypersensitivity-hyperesthesia-dissociative phenomena-etc. ) . 
The invention also relates to methods comprising administering to a 
patient diagnosed as having a neuropsychiatric disorder a pharmaceutical 
compn. contg. (i) compds. having D4 antagonistic, partial agonistic or 
inverse agonistic activity and (ii) compds. having 5-HT2A antagonistic, 
partial agonistic or inverse agonistic, and (iii) any known medicinal 
compd. and compns. of said compds. The combined D4 and 5-HT2A 
antagonistic, partial agonistic or inverse agonistic effects may reside 
within the same chem. or biol. compd. or in two different chem. and/or 



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biol . compds . 
IT 93413-62-8 / Desvenlaf axine 

RL: PAC (Pharmacological activity); THU (Therapeutic use) ; BIOL 

(Biological study); USES (Uses) 

(use of D4 and 5-HT2A antagonists or inverse agonists or partial 
agonists in treatment of emotional dysregulation in mental disorders 
combined with other agents) 
RN 93413-62-8 HCAPLUS 

CN Phenol, 4- [2- (dimethylamino) -1- (1-hydroxycyclohexyl) ethyl] - (901) (CA 
INDEX NAME) 



HO 

L4 



Me 2N-CH2 




OH 



ANSWER 3 OF 38 HCAPLUS COPYRIGHT 2005 ACS on STN 



ACCESSION NUMBER: 
DOCUMENT NUMBER: 
TITLE: 

INVENTOR (S) : 

PATENT ASSIGNEE (S) : 
SOURCE : 

DOCUMENT TYPE: 
LANGUAGE : 

FAMILY ACC. NUM. COUNT: 
PATENT INFORMATION: 



2005 : 735104 HCAPLUS 

143: 199895 

Multiparticulate 0-desmethylvenlaf axine salts and uses 
thereof 

Diorio, Christopher Richard; Shah, Syed M. ; Fawzi, 
Mahdi B. 

Wyeth, John, and Brother Ltd., USA 
U.S. Pat . Appl , Publ . , 7 pp . 

CODEN : USXXCO 

Patent 

English 

1 



PATENT NO. 



KIND 



DATE 



APPLICATION NO. 



DATE 



US 2005175698 




Al 




20050811 




US 2005- 


42436 




20050125 


WO 2005077340 




Al 




20050825 




WO 2005- 


US2215 




20050125 


W: 


AE, 


AG, 


AL, 


AM, 


AT, 


AU, 


AZ, 


BA, 


BB, 


BG, 


BR, 


BW, 


BY, 


BZ, 


CA, CH, 




CN, 


CO, 


CR, 


CU, 


CZ, 


DE, 


DK, 


DM, 


DZ, 


EC, 


EE, 


EG, 


ES, 


FI, 


GB, GD, 




GE, 


GH, 


GM, 


HR, 


HU, 


ID, 


IL, 


IN, 


IS, 


JP, 


KE, 


KG, 


KP, 


KR, 


KZ, LC, 




LK, 


LR, 


LS, 


LT, 


LU, 


LV, 


MA, 


MD, 


MG, 


MK, 


MN, 


MW, 


MX, 


MZ, 


NA, NI, 




NO, 


NZ, 


OM, 


PG, 


PH, 


PL, 


PT, 


RO, 


RU, 


SC, 


SD, 


SE, 


SG, 


SK, 


SL, SY, 




TJ, 


TM, 


TN, 


TR, 


TT, 


TZ, 


UA, 


UG, 


US, 


uz. 


vc. 


VN, 


YU, 


ZA, 


ZM, ZW 


RW: 


BW, 


GH, 


GM, 


KE, 


LS, 


MW, 


MZ, 


NA, 


SD, 


SL, 


sz. 


TZ, 


UG, 


ZM, 


ZW, AM, 




AZ, 


BY, 


KG, 


KZ, 


MD, 


RU, 


TJ, 


TM, 


AT, 


BE, 


BG, 


CH, 


CY, 


CZ, 


DE, DK, 




EE, 


ES, 


FI, 


FR, 


GB, 


GR, 


HU, 


IE, 


IS, 


IT, 


LT, 


LU, 


MC, 


NL, 


PL, PT, 




RO, 


SE, 


SI, 


SK, 


TR, 


BF, 


BJ, 


CF, 


CG, 


CI, 


CM, 


GA, 


GN, 


GQ, 


GW, ML, 




MR, 


NE, 


SN, 


TD, 


TG 






















PRIORITY APPLN. 


INFO 














US 2004- 


542384P 




P 20040206 



AB 



A multiparticulate o-desmethylvenlaf axine (ODV) succinate or formate is 
described. Methods of treating depression and reducing the 
gastrointestinal side-effects of ODV are also described. 
IT 93413-62-8D , O-Desmethylvenlaf axine, salts 448904-47-0 
861972-83-0 

RL: PEP (Physical, engineering or chemical process); PYP (Physical 
process); THU (Therapeutic use) ; BIOL (Biological study); PROC 
(Process); USES (Uses) 

(multiparticulate O-desmethylvenlaf axine salts and uses thereof) 



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RN 93413-62-8 HCAPLUS 

CN Phenol, 4- [2- { dime thylamino) -1- ( 1-hydroxycyclohexyl ) ethyl] - {9CI) (CA 
INDEX NAME) 



RN 448904-47-0 HCAPLUS 

CN Butanedioic acid, compd, with 4- [2- (dimethylamino) -1- (l- 
hydroxycyclohexyl) ethyl] phenol (1:1) (9CI) (CA INDEX NAME) 

CM 1 

CRN 93413-62-8 
CMF C16 H25 N 02 



^:Me2N-CH2 



CM 2 

CRN 110-15-6 
CMF C4 H6 04 



RN 861972-83-0 HCAPLUS 

CN Formic acid, compd. with 4- [2- (dimethylamino) -1- ( 1- 

hydroxycyclohexyl) ethyl] phenol (1:1) (9CI) (CA INDEX NAME) 

CM 1 

CRN 93413-62-8 
CMF C16 H25 N 02 



Me 2M-CH2 






CM 



2 



CRN 
CMF 



64-18-6 
C H2 02 



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L4 ANSWER 4 OF 38 HCAPLUS COPYRIGHT 2005 ACS on STN 



Full 1 




Text 1 


^fsrene^ 1 



ACCESSION NUMBER: 
DOCUMENT NUMBER: 
TITLE: 



INVENTOR (S) : 

PATENT ASSIGNEE (S) : 
SOURCE : 

DOCUMENT TYPE: 
LANGUAGE : 

FAMILY ACC. NUM. COUNT: 
PATENT INFORMATION: 



2005:588665 HCAPLUS 
143:103256 

Combination of a sedative and a neurotransmitter 
modulator for improving sleep quality and treating 
depression 

Lalji, Karim; Barberich, Timothy J.; Caron, Judy; 

Wessel, Thomas 

Sepracor Inc., USA 

PCT Int. Appl., 394 pp. 

CODEN: PIXXD2 

Patent 

English 

1 



PATENT NO. 






KIND 


DATE 






APPLICATION : 


NO. 




DATE 


WO 2005060968 




Al 




20050707 




WO 2004- 


US40962 




20041208 


W: AE, 


AG, 


AL, 


AM, 


AT, 


AU, 


AZ, 


BA, 


BB, BG, 


BR, 


BW, 


BY, 


BZ , OA, CH , 


CN, 


CO, 


CR, 


CU, 


CZ, 


DE, 


DK, 


DM, 


DZ, EC, 


EE, 


EG, 


ES, 


FI, GB, GD, 


GE, 


GH, 


GM, 


HR, 


HU, 


ID, 


IL, 


IN, 


IS, JP, 


KE, 


KG, 


KP, 


KR, KZ , LC, 


LK, 


LR, 


LS, 


LT, 


LU, 


LV, 


MA, 


MD, 


MG, MK, 


MN, 


MW, 


MX, 


MZ, NA, NI, 


NO, 


NZ, 


OM, 


PG, 


PH, 


PL, 


PT, 


RO, 


RU, SC, 


SD, 


SE, 


SG, 


SK, SL, SY, 


TJ, 


TM, 


TN, 


TR, 


TT, 


TZ, 


UA, 


UG, 


US, UZ, 


vc. 


VN, 


YU, 


ZA, ZM, ZW 


RW: BW, 


GH, 


GM, 


KE, 


LS, 


MW, 


MZ, 


NA, 


SD, SL, 


sz. 


TZ, 


UG, 


ZM, ZW, AM, 


AZ, 


BY, 


KG, 


KZ, 


MD, 


RU, 


TJ, 


TM, 


AT, BE, 


BG, 


CH, 


CY, 


CZ, DE, DK, 


EE, 


ES, 


FI, 


FR, 


GB, 


GR, 


HU, 


IE, 


IS, IT, 


LT, 


LU, 


MC, 


NL, PL, PT, 


RO, 


SE, 


SI, 


SK, 


TR, 


BF, 


BJ, 


CF, 


CG, CI, 


CM, 


GA, 


GN, 


GQ, GW, ML, 


MR, 


NE, 


SN, 


TD, 


TG 


















US 2005176680 




Al 




20050811 




US 2004- 


7795 






20041208 


PRIORITY APPLN. 


INFO 














US 2003- 


529156P 




P 20031211 


















US 2004- 


541614P 




P 20040204 


















US 2004- 


633213P 




P 20041203 



AB One aspect of the present invention relates to pharmaceutical compns . 

contg. 2 or more active agents that when taken together can be used to 
treat, e.g., insomnia and/or depression. The first component of the 
pharmaceutical compn. is a GABA receptor modulating compd. The second 
component of the pharmaceutical compn. is a serotonin reuptake inhibitor 
(SRI), a norepinephrine reuptake inhibitor (NRI), a 5-HT2A modulator, or 
dopamine reuptake inhibitor (DRI) . In certain embodiments, the 
pharmaceutical compn. comprises eszopiclone. In a preferred embodiment, 
the pharmaceutical compn. comprises eszopiclone and fluoxetine. The 
present invention also relates to a method of treating a sleep 
abnormality, treating insomnia, treating depression, augmenting 
antidepressant therapy, eliciting a dose-sparing effect, reducing 
depression relapse, improving the efficacy of antidepressant therapy or 
improving the tolerability of antidepressant therapy, comprising 
co-administering to a patient in need thereof a GABA- receptor-modulating 
compd.; and a SRI, NRI, 5-HT2A modulator or DRI. Co-administration of 
eszopiclone with fluoxetine was well-tolerated and assocd. with rapid, 
sustained improvement in sleep and daytime symptoms in patients with MDD 
and insomnia. The rapid sleep improvement with adjunctive eszopiclone may 
be important, given the relatively slower onset of antidepressant effects 
with SSRIs. 

IT 93413-62-8 142761-11-3 142761-12-4 

RL: PAC (Pharmacological activity); THU (Therapeutic use) ; BIOL 
(Biological study); USES (Uses) 



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(combination of sedative and neurotransmitter modulator for improving 
sleep quality and treating depression) 
RN 93413-62-8 HCAPLUS 

CN Phenol, 4- [2- (dimethyl ami no) -1- (1-hydroxycyclohexyl) ethyl] - (9CI) (CA 
INDEX NAME) 



HO 



Me 2W-CH2 




OH 



RN 142761-11-3 HCAPLUS 

CN Phenol, 4-[ ( IR) -2- (dimethylamino) -1- ( 1-hydroxycyclohexyl) ethyl] - (9CI) 
(CA INDEX NAME) 

Absolute stereochemistry. Rotation (-) . 



Nile 2 




RN 142761-12-4 HCAPLUS 

CN Phenol, 4-[ (IS) -2- (dimethylamino) -1- ( 1-hydroxycyclohexyl) ethyl] - (9CI) 
(CA INDEX NAME) 

Absolute stereochemistry. Rotation (+) . 



NMe2 




REFERENCE COUNT: 



THERE }\RE 1 CITED REFERENCES AVAIL7\BLE FOR THIS 
RECORD. ALL CITATIONS AVAILABLE IN THE RE FORMAT 



ANSWER 5 OF 38 HCAPLUS COPYRIGHT 2005 ACS on STN 




ACCESSION NUMBER: 
DOCUMENT NUMBER: 
TITLE: 

INVENTOR (S) : 
PATENT ASSIGNEE (S) : 
SOURCE : 

DOCUMENT TYPE: 
LANGUAGE : 

FAMILY ACC. NUM. COUNT: 
PATENT INFORMATION: 



2005:517402 HCAPLUS 
143:38422 

Combination therapy for dementia, depression and 
apathy 

Sheldon, Leslie James 
Can. 

PCT Int. Appl., 47 pp. 

CODEN: PIXXD2 

Patent 

English 

1 



PATENT NO. 



KIND DATE 



APPLICATION NO. 



DATE 



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2005053703 




Al 




20050616 




WO 2004- 


CA2071 




20041202 


W: AE, 


AG, 


AL, 


AM, 


AT, 


AU, 


AZ, 


BA, 


BB, 


BG, 


BR, 


BW, 


BY, 


BZ, 


CA, CH, 


CN, 


CO, 


CR, 


CU, 


CZ, 


D£, 


DK, 


DM, 




EC, 


EE, 


EG, 


ES, 


FI, 


GB, GD, 


GE, 


GH, 


GM, 


HR, 


HU, 


ID, 


T T 

IL, 


IN, 


IS, 


JP, 


KE, 


KG, 


KP, 


KR, 


KZ, LC, 


LK, 


LR, 


LS, 


LT, 


LU, 


LV, 


MA, 


MD, 


MG, 


MK, 


MN, 


MW, 


MX, 


MZ , 


NA, NI , 


NO, 


NZ , 


OM, 


PG, 


PH, 


PL, 


PT, 


RO, 


RU, 


SC, 


SD, 


SE, 


SG, 


SK, 


SL, SY, 


TJ, 


TM, 


TN, 


TR, 


TT, 


TZ, 


UA, 


UG, 


us. 


UZ, 


VC, 


VN, 


YU, 


ZA, 


ZM, ZW 


RW: BW, 


GH, 


GM, 


KE, 


LS, 


MW, 


MZ, 


NA, 


SD, 


SL, 


SZ, 


TZ, 


UG, 


ZM, 


ZW, AM, 


AZ, 


BY, 


KG, 


KZ, 


MD, 


RU, 


TJ, 


TM, 


AT, 


BE, 


BG, 


CH, 


CY, 


CZ, 


DE, DK, 


EE, 


ES, 


FI, 


FR, 


GB, 


GR, 


HU, 


IE, 


IS, 


IT, 


LT, 


LU, 


MC, 


NL, 


PL, PT, 


RO, 


SE, 


SI, 


SK, 


TR, 


BF, 


BJ, 


CF, 


CG, 


CI, 


CM, 


GA, 


GN, 


GQ, 


GW, ML, 


MR, 


NE, 


SN, 


TD, 


TG 






















APPLN. 


INFO 














US 2003- 


526137P 




P 20031202 



AB The invention provides compns. and kits for treating dementia, depression 
and apathy using combination therapy involving either a monoamine oxidase 
inhibitor or a selective serotonin reuptake inhibitor in combination with 
an anti-psychotic agent. 

IT 93413-62-8 , Desvenlaf axine 

RL: PAC (Pharmacological activity); THU (Therapeutic use); BIOL 
(Biological study) ; USES (Uses) 

(combination therapy for dementia, depression and apathy) 

RN 93413-62-8 HCAPLUS 

CN Phenol, 4~ [2- (dimethyl amino) -1- ( 1-hydroxycyclohexyl) ethyl] - (SCI) (CA 
INDEX NAME) 



HO 



Me 2N-CH2 




OH 



REFERENCE COUNT: 



14 THERE ARE 14 CITED REFERENCES AVAILABLE FOR THIS 
RECORD. ALL CITATIONS AVAILABLE IN THE RE FORMAT 



L4 ANSWER 6 OF 38 HCAPLUS COPYRIGHT 2005 ACS on STN 



ACCESSION NUMBER: 
DOCUMENT NUMBER: 
TITLE: 

INVENTOR (S) : 
PATENT ASSIGNEE (S) : 
SOURCE : 

DOCUMENT TYPE: 
LANGUAGE : 

FAMILY ACC. NUM. COUNT: 
PATENT INFORMATION: 



2005: 516281 HCAPLUS 
143:38421 

Use of D4 and 5-HT2A antagonists, inverse agonists or 

partial agonists 

Buntinx, Erik 

B&B Beheer N. V., Belg. 

Eur. Pat. Appl., 145 pp. 

CODEN: EPXXDW 

Patent 

English 

6 



PATENT NO. 



KIND 



DATE 



APPLICATION NO. 



DATE 



EP 


1541197 






Al 




20050615 




EP 2004- 


25035 




20041021 




R: AT, 


BE, 


CH, 


DE, 


DK, 


ES, FR, 


GB, 


GR, IT, 


LI, LU, 


NL, 


SE, MC, PT, 




IE, 


SI, 


LT, 


LV, 


FI, 


RO, MK, 


CY, 


AL, TR, 


BG, CZ, 


EE, 


HU, PL, SK, 


EP 


1547650 






Al 




20050629 




EP 2003- 


447279 




20031202 




R: AT, 


BE, 


CH, 


DE, 


DK, 


ES, FR, 


GB, 


GR, IT, 


LI, LU, 


NL, 


SE, MC, PT, 




IE, 


SI, 


LT, 


LV, 


FI, 


RO, MK, 


CY, 


AL, TR, 


BG, CZ, 


EE, 


HU, SK 


EP 


1576985 






Al 




20050921 




EP 2004- 


447066 




20040318 




R: AT, 


BE, 


CH, 


DE, 


DK, 


ES, FR, 


GB, 


GR, IT, 


LI, LU, 


NL, 


SE, MC, PT, 



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11/22/05 



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IE, 


SI, 


LT, 


LV, 


FI, 


RO, 


MK, 


CY, 


AL, TR, 


BG, CZ, 


EE, 


HU, PL, SK 


JP 


2005194263 




A2 




20050721 




JP 2004- 


349085 




20041104 


us 


2005203130 




Al 




20050915 




US 2004- 


984683 




20041109 


CA 


2487529 






AA 




20050602 




CA 2004- 


2487529 




20041115 


WO 


2005053796 




Al 




20050616 




WO 2004- 


BE172 




20041202 




w : / 




AL, 


AM, 


AT, 


T\TT 


TV 


BA, 


BB, BG, 


BR, BW, 


BY, 


BZ, CA, CH 








CR, 


CU, 


CZ, 




JJK, 


DM, 


DZ, EC, 


EE, EG, 


ES, 


FI, GB, GD 




GE, 


GH, 


GM, 


HR, 


HU, 


ID, 


IL, 


IN, 


IS, JP, 


KE, KG, 


KP, 


KR, KZ, LC 




LK, 


LR, 


LS, 


LT, 


LU, 


LV, 


MA, 


MD, 


MG, MK, 


MN, MW, 


MX, 


MZ, NA, NI 




NO, 


NZ, 


OM, 


PG, 


PH, 


PL, 


PT, 


RO, 


RU, SC, 


SD, SE, 


SG, 


SK, SL, SY 




TJ, 


TM, 


TN, 


TR, 


TT, 


TZ, 


UA, 


UG, 


US, UZ, 


VC, VN, 


YU, 


ZA, ZM, ZW 




RW: BW, 


GH, 


GM, 


KE, 


LS, 


MW, 


MZ, 


NA, 


SD, SL, 


SZ, TZ, 


UG, 


ZM, ZW, AM 




AZ, 


BY, 


KG, 


KZ, 


MD, 


RU, 


TJ, 


TM, 


AT, BE, 


BG, CH, 


CY, 


CZ, DE, DK 




EE, 


ES, 


FI, 


FR, 


GB, 


GR, 


HU, 


IE, 


IS, IT, 


LT, LU, 


MC, 


NL, PL, PT 




RO, 


SE, 


SI, 


SK, 


TR, 


BF, 


BJ, 


CF, 


CG, CI, 


CM, GA, 


GN, 


GQ, GW, ML 




MR, 


NE, 


SN, 


TD, 


TG 
















RITY APPLN. 


INFO 


• * 












EP 2003- 


447279 




A 20031202 




















EP 2004- 


447001 




A 20040105 




















EP 2004- 


447066 




A 20040318 




















CA 2003- 


2451798 




A 20031202 




















US 2003- 


725965 




A2 20031202 




















US 2004- 


752423 




A2 20040106 




















CA 2004- 


2461248 




A 20040318 




















US 2004- 


803793 




A2 20040318 




















EP 2004- 


25035 




A 20041021 




















JP 2004- 


349085 




A 20041104 




















US 2004- 


984683 




A 20041109 




















CA 2004- 


2487529 




A 20041115 



AB The present invention relates to the use of compds . and compns. of compds . 
having D4 and 5-HT2A antagonistic, partial agonistic or inverse agonistic 
activity for the treatment of the underlying dysregulation of the 
emotional functionality of mental disorders (i.e. affect 

instability-hypersensitivity-hyperesthesia-dissociative phenomena-etc. ) . 
The invention also relates to methods comprising administering to a 
patient diagnosed as having a neuropsychiatric disorder a pharmaceutical 
compn. contg. (i) compds. having D4 antagonistic, partial agonistic or 
inverse agonistic activity and (ii) compds. having 5-HT2A antagonistic, 
partial agonistic or inverse agonistic, and (iii) any known medicinal 
compd. and compns. of said compds. The combined D4 and 5-HT2A 
antagonistic, partial agonistic or inverse agonistic effects may reside 
within the same chem. or biol. compd. or in two different chem. and/or 
biol. compds. 

IT 93413-62-8 , Desvenlaf axine 

RL: PAC (Pharmacological activity); THU (Therapeutic use); BIOL 
(Biological study); USES (Uses) 

(use of D4 and 5-HT2A antagonists or inverse agonists or partial 
agonists in treatment of emotional dysregulation in mental disorders 
combined with other agents) 

RN 93413-62-8 HCAPLUS 

CN Phenol, 4- [2- (dimethylamino) -1- ( 1-hydroxycyclohexyl) ethyl] - (9CI) (CA 
INDEX NAME) 




REFERENCE COUNT: 24 THERE ARE 24 CITED REFERENCES AVAILABLE FOR THIS 



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RECORD. ALL CITATIONS AVAILABLE IN THE RE FORMAT 



r-yu\\ — 1 




Text 1 





L4 ANSWER 7 OF 38 HCAPLUS COPYRIGHT 2005 ACS on STN 



2005 : 493467 HCAPLUS 
143:38409 

Combination drug therapy to treat obesity 

Seed, John C. 

USA 

PCT Int. Appl., 47 pp. 

CODEN: PIXXD2 

Patent 

English 

1 



ACCESSION NUMBER: 
DOCUMENT NUMBER: 
TITLE : 

INVENTOR (S) : 
PATENT ASSIGNEE (S) : 
SOURCE : 

DOCUMENT TYPE: 
LANGUAGE : 

FAMILY ACC. NUM. COUNT: 
PATENT INFORMATION: 



PATENT NO. KIND DATE APPLICATION NO. DATE 



WO 2005051297 




A2 




20050609 




WO 2004- 


US38981 




20041119 


W: AE, 


AG, 


AL, 


AM, 


AT, 


AU, 


AZ, 


BA, 


BB, 


BG, 


BR, 


BW, 


BY, 


BZ, CA, CH, 


CN, 


CO, 


. CR, 


CU, 


CZ, 


DE, 


DK, 


DM, 


DZ, 


EC, 


EE, 


EG, 


ES, 


FI, GB, GD, 


GE, 


GH, 


GM, 


HR, 


HU, 


ID, 


IL, 


IN, 


IS, 


JP, 


KE, 


KG, 


KP, 


KR , KZ, LC, 


LK, 


LR, 


LS, 


LT, 


LU, 


LV, 


MA, 


MD, 


MG, 


MK, 


MN, 


MW, 


MX, 


MZ, NA, NI, 


NO, 


NZ, 


OM, 


PG, 


PH, 


PL, 


PT, 


RO, 


RU, 


SC, 


SD, 


SE, 


SG, 


SK, SL, SY, 


TJ, 


TM, 


TN, 


TR, 


TT, 


TZ, 


UA, 


UG, 


US, 


UZ, 


vc. 


VN, 


YU, 


ZA, ZM, ZW 


RW: BW, 


GH, 


GM, 


. KE, 


LS, 


MW, 


MZ, 


NA, 


SD, 


SL, 


SZ, 


TZ, 


UG, 


ZM, ZW, AM, 


AZ, 


BY, 


KG, 


KZ, 


MD, 


RU, 


TJ, 


TM, 


AT, 


BE, 


BG, 


CH, 


CY, 


CZ, DE, DK, 


EE, 


ES, 


FI, 


FR, 


GB, 


GR, 


HU, 


IE, 


IS, 


IT, 


LU, 


MC, 


NL, 


PL, PT, RO, 


SE, 


SI, 


SK, 


TR, 


BF, 


BJ, 


CF, 


CG, 


CI, 


CM, 


GA, 


GN, 


GQ, 


GW, ML, MR, 


NE, 


SN, 


TD, 


TG 






















US 2005143350 




Al 




20050630 




US 2004- 


993496 




20041118 


PRIORITY APPLN. 


INFO 














US 2003- 


523610P 




P 20031119 


















US 2004- 


993496 




A 20041118 



AB Provided are methods of achieving desirable wt. loss in an overweight or 
obese individual by administering at least one anticholinesterase agent 
and at least one antidepressant. The invention also provides for 
pharmaceutical compns. and kits for simultaneous delivery of at least one 
anticholinesterase agent and at least one antidepressant. 

IT 93413-62-8 , Desvenlaf axine 142761-11-3 
142761-12-4 

RL: PAC (Pharmacological activity); THU (Therapeutic use); BIOL 
(Biological study); USES (Uses) 

(combination drug therapy to treat obesity) 
RN 93413-62-8 HCAPLUS 

CN Phenol, 4- [2- (dimethyl ami no) -1- ( 1-hydroxycyclohexyl) ethyl] - (9CI) (CA 
INDEX NAME) 




RN 142761-11-3 HCAPLUS 

CN Phenol, 4- [ ( IR) -2- (dimethylamino) -1- { 1-hydroxycyclohexyl) ethyl] - (9CI) 
(CA INDEX NAME) 

Absolute stereochemistry. Rotation (-) . 



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11/22/05 



Page 13 of 51 




RN 142761-12-4 HCAPLUS 

CN Phenol, 4-[ ( IS ) --2- (dimethylamino) -1- { 1-hydroxycyclohexyl) ethyl] - (9CI) 
(CA INDEX NAME) 

Absolute stereochemistry. Rotation (+) . 




ANSWER 8 OF 38 HCAPLUS COPYRIGHT 2005 ACS on STN 




ACCESSION NUMBER: 
DOCUMENT NUMBER: 
TITLE: 



INVENTOR (S) : 

PATENT ASSIGNEE (S) : 
SOURCE : 

DOCUMENT TYPE: 
LANGUAGE : 

FAMILY ACC. NUM. COUNT: 
PATENT INFORMATION: 



2005:369266 HCAPLUS 
142:404276 

Method using adrenergic a2B antagonists, alone 
or in combination with norepinephrine reuptake 
inhibitors or dual norepinephrine/serotonin reuptake 
inhibitors for treating vasomotor symptoms 
Deecher, Darlene Coleman; Beyer, Chad Edward; 
Leventhal, Liza 

Wyeth, John, and Brother Ltd., USA 

PCT Int. Appl., 48 pp. 

CODEN : PIXXD2 

Patent 

English 

3 



PATENT NO. KIND DATE APPLICATION NO. DATE 



WO 


20050372 


60 




A2 




20050428 




WO 2004- 


US33754 




20041013 




W: AE, 


AG, 


AL, 


AM, 


AT, 


AU, 


AZ, 


BA, 


BB, 


BG, 


BR, 


BW, 


BY, 


BZ, 


CA, CH, 




CN, 


CO, 


CR, 


CU, 


CZ, 


DE, 


DK, 


DM, 


DZ, 


EC, 


EE, 


EG, 


ES, 


FI, 


GB, GD, 




GE, 


GH, 


GM, 


HR, 


HU, 


ID, 


IL, 


IN, 


IS, 


JP, 


KE, 


KG, 


KP, 


KR, 


KZ, LC, 




LK, 


LR, 


LS, 


LT, 


LU, 


LV, 


MA, 


MD, 


MG, 


MK, 


MN, 


MW, 


MX, 


MZ, 


NA, NI, 




NO, 


NZ, 


OM, 


PG, 


PH, 


PL, 


PT, 


RO, 


RU, 


SC, 


SD, 


SE, 


SG, 


SK, 


SL, SY, 




TJ, 


TM, 


TN, 


TR, 


TT, 


TZ, 


UA, 


UG, 


US, 


uz. 


vc. 


VN, 


YU, 


ZA, 


ZM, ZW 




RW: BW, 


GH, 


GM, 


KE, 


LS, 


MW, 


MZ, 


NA, 


SD, 


SL, 


sz. 


TZ, 


UG, 


ZM, 


ZW, AM, 




AZ, 


BY, 


KG, 


KZ, 


MD, 


RU, 


TJ, 


TM, 


AT, 


BE, 


BG, 


CH, 


CY, 


CZ, 


DE, DK, 




EE, 


ES, 


FI, 


FR, 


GB, 


GR, 


HU, 


IE, 


IT, 


LU, 


MC, 


NL, 


PL, 


PT, 


RO, SE, 




SI, 


SK, 


TR, 


BF, 


BJ, 


CF, 


CG, 


CI, 


CM, 


GA, 


GN, 


GQ, 


GW, 


ML, 


MR, NE, 




SN, 


TD, 


TG 


























US 


2004152710 




Al 




20040805 




US 2003- 


685812 




20031014 


wo 


2004035058 




Al 




20040429 




WO 2003- 


US32759 




20031015 




W: AE, 


AG, 


AL, 


AM, 


AT, 


AU, 


AZ, 


BA, 


BB, 


BG, 


BR, 


BY, 


BZ, 


CA, 


CH, CN, 




CO, 


CR, 


CU, 


CZ, 


DE, 


DK, 


DM, 


DZ, 


EC, 


EE, 


EG, 


ES, 


FI, 


GB, 


GD, GE, 




GH, 


GM, 


HR, 


HU, 


ID, 


IL, 


IN, 


IS, 


JP, 


KE, 


KG, 


KP, 


KR, 


KZ, 


LC, LK, 




LR, 


LS, 


LT, 


LU, 


LV, 


MA, 


MD, 


MG, 


MK, 


MN, 


MW, 


MX, 


MZ, 


NO, 


NZ, OM, 



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PG, 


PH, 


PL, 


PT, 


RO, 


RU, 


SC, 


SD, 


SE, SG, 


SK, SL, 


SY, 


TJ, TM, TN, 


TR, 


TT, 


TZ, 


UA, 


UG, 


US, 


UZ, 


VC, 


VN, YU, 


ZA, ZM, 


ZW 




RW: GH, 


GM, 


K£, 


LS, 


MW, 


MZ, 


SD, 


SL, 


SZ, TZ, 


UG, ZM, 


ZW, 


AM, AZ, BY, 


KG, 


KZ, 


MD, 


RU, 


TJ, 


TM, 


AT, 


BE, 


BG, CH, 


CY, CZ, 


DE, 


DK, EE, ES, 


FI, 


FR, 


GB, 


GR, 


HU, 


IE, 


IT, 


LU, 


MC, NL, 


PT, RO, 


SE, 


SI, SK, TR, 


BF, 


BJ, 


CF, 


CG, 


CI, 


CM, 


GA, 


GN, 


GQ, GW, 


ML, MR, 


NE, 


SN, TD, TG 


US 2005130987 




Al 




20050616 




US 2004- 


962897 




20041012 


PRIORITY APPLN. 


INFO 














US 2003- 


510897P 




P 20031014 


















US 2003- 


685812 




A 20031014 


















WO 2003- 


US32759 




A 20031015 


















US 2004- 


962897 




A 20041012 


















US 2002- 


418591P 




P 20021015 



AB The invention discloses selective adrenergic a2B antagonists alone, 
selective adrenergic a2B antagonists in combination with 
norepinephrine reuptake inhibitors (NRI) (as a single compd. or as a 
combination of two or more compds.)/ or selective adrenergica2B 
antagonists in combination with dual norepinephrine reuptake 
inhibitors/serotonin reuptake inhibitors (NRI/SRI) (as a single compd. or 
as a combination of two or more compds.) and methods of their use in the 
treatment of vasomotor symptoms. 

IT 93413-62-8 , 0-Desmethylvenlaf axine 

RL: PAG (Pharmacological activity); THU (Therapeutic use); BIOL 
(Biological study); USES (Uses) 

(adrenergic a2B antagonists, alone or in combination with 
norepinephrine reuptake inhibitors or dual norepinephrine/serotonin 
reuptake inhibitors for treating vasomotor symptoms) 

RN 93413-62-8 HCAPLUS 

CN Phenol, 4- [2- (dimethylamino) -1- (1-hydroxycyclohexyl) ethyl] - (9CI) (OA 
INDEX NAME) 



HO 



Me2N-CH2 




'-0 



OH 



L4 ANSWER 9 OF 38 HCAPLUS COPYRIGHT 2005 ACS on STN 



HCAPLUS 



ACCESSION NUMBER: 
DOCUMENT NUMBER: 
TITLE: 

INVENTOR (S) : 

PATENT ASSIGNEE (S) : 
SOURCE : 

DOCUMENT TYPE: 
LANGUAGE : 

FAMILY ACC. NUM. COUNT: 
PATENT INFORMATION: 



2005:340220 
142:360912 

Extended release pharmaceutical dosage form 

Heaton, Nicholas; Potts, Angela; Armstrong, Ian; 

Provost, James J^ndrew 

Wyeth, John, and Brother Ltd., USA 

Eur. Pat. Appl., 12 pp. 

CODEN: EPXXDW 

Patent 

English 

1 



PATENT NO. 



EP 1523979 



KIND DATE 



Al 



20050420 



APPLICATION NO. 



EP 2003-256438 



DATE 



20031013 



R: AT, BE, CH, DE, DK, ES, FR, GB, GR, IT, LI, LU, NL, SE, MC, PT, 
IE, SI, LT, LV, FI, RO, MK, CY, AL, TR, BG, CZ, EE, HU, SK 
WO 2005039527 A2 20050506 WO 2004-EP11339 20041011 



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Page 15 of 51 



W: 




AG, 


AL, 


AM, 


AT, 


AU, 


AZ, 


BA, 


BB, 


BG, 


BR, 


BW, 


BY, 


BZ, 


CA, 


CH, 




CN, 


CO, 


CR, 


CU, 


CZ, 


DE, 


DK, 


DM, 


DZ, 


EC, 


EE, 


EG, 


ES, 


FI, 


GB, 


GD, 




GE, 


GH, 


GM, 


HR, 


HU, 


ID, 


IL, 


IN, 


IS, 


JP, 


KE, 


KG, 


KP, 


KR, 


KZ, 


LC, 




LK, 


LR, 


LS, 


LT, 


LU, 


LV, 


MA, 


MD, 


MG, 


MK, 


MN, 


MW, 


MX, 


MZ, 


NA, 


NI, 




NO, 


NZ, 


OM, 


PG, 


PH, 


PL, 


PT, 


RO, 


RU, 


SC, 


SD, 


SE, 


SG, 


SK, 


SL, 


SY, 




TJ, 


TM, 


TN, 


TR, 


TT, 


TZ, 


UA, 


UG, 


US, 


UZ, 


vc, 


VN, 


YU, 


ZA, 


ZM, 


zw 


RW: 


BW, 


GH, 


GM, 


KE, 


LS, 


MW, 


MZ, 


NA, 


SD, 


SL, 


sz. 


TZ, 


UG, 


ZM, 


zw. 


AM, 




AZ, 


BY, 


KG, 


KZ, 


MD, 


RU, 


TJ, 


TM, 


AT, 


BE, 


BG, 


CH, 


CY, 


CZ, 


DE, 


DK, 




EE, 


ES, 


FI, 


FR, 


GB, 


GR, 


HU, 


IE, 


IT, 


LU, 


MC, 


NL, 


PL, 


PT, 


RO, 


SE, 




SI, 


SK, 


TR, 


BF, 


BJ, 


CF, 


CG, 


CI, 


CM, 


GA, 


GN, 


GQ, 


GW, 


ML, 


MR, 


NE, 



SN, TD, TG 

US 2005129762 Al 20050616 US 2004-964012 20041013 

PRIORITY APPLN. INFO.: EP 2003-256438 A 20031013 

AB This invention relates to novel extended release pharmaceutical dosage 
forms for orally delivering drugs to mammals, e.g., humans. More 
particularly, this invention concerns novel dosage forms of water sol. 
drugs such as venlafaxine, enantiomeric (R or S) forms of venlafaxine, 
metabolites of venlafaxine such as 0-desmethyl venlafaxine (ODV) or 
enantiomeric (R or S) forms of said metabolites which dosage forms have an 
extended release profile when taken orally. This invention also provides 
processes for prepg, such dosage forms and methods of using them. For 
example, extended-release tablets of venlafaxine hydrochloride comprised 
(1) a tablet core contg. venlafaxine HCl 81.45, stearic acid 96.55, 
microcryst. cellulose 20, colloidal silica 0.4, Mg stearate 1 . 6 mg and (2) 
a coating layer contg. venlafaxine HCl 3.89 and stearic acid 16.97 mg. 
IT 142761-11-3 , (-)-O-DesmethylVenlafaxine 142761-12-4 , 
(+) -O-Desmethyl Venlafaxine 

RL: PKT (Pharmacokinetics); THU (Therapeutic use) ; BIOL 
(Biological study); USES (Uses) 

(extended release oral dosage forms of venlafaxine enantiomers and 

metabolites) 
RN 142761-11-3 HCAPLUS 

CN Phenol, 4- [ ( IR) -2- (dimethylamino) -1- ( 1-hydroxycyclohexyl) ethyl] - (9CI) 
(CA INDEX NAME) 

Absolute stereochemistry. Rotation (-) . 




RN 142761-12-4 HCAPLUS 

CN Phenol , 4- [ ( IS ) -2- (dimethyl amino ) - 1- ( 1-hydroxycyclohexyl ) ethyl ] - { 9CI ) 
(CA INDEX NAME) 

Absolute stereochemistry. Rotation (+) . 



OK. 

4 THERE ARE 4 CITED REFERENCES AVAILABLE FOR THIS 

RECORD. ALL CITATIONS AVAILABLE IN THE RE FORMAT 




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ANSWER 10 OF 38 

il 

ACCESSION NUMBER: 
DOCUMENT NUMBER: 
TITLE: 



INVENTOR (S) : 

PATENT ASSIGNEE (S) : 
SOURCE : 

DOCUMENT TYPE: 
LANGUAGE : 

FAMILY ACC. NUM. COUNT: 
PATENT INFORMATION: 



HCAPLUS COPYRIGHT 2005 ACS on STN 



2005 : 238701 HCAPLUS 
142:316826 

A preparation of combinations comprising alpha-2-delta 
ligands and dual serotonin-noradrenaline reuptake 
inhibitors, useful for treatment of pain 
Dooley, David James; Field, Mark John; Williams, 
Richard Griffith 
USA 

U.S. Pat. Appl. Publ., 23 pp. 

CODEN: USXXCO 

Patent 

English 

1 



PATENT NO. 



KIND DATE 



APPLICATION NO. 



DATE 



US 


2005059715 




Al 




20050317 




US 2004- 


935824 




20040908 


WO 


2005025675 




Al 




20050324 




WO 2004- 


IB2943 




20040906 




W: 


AE, 


AG, 


AL, 


AM, 


AT, 


AU, 


AZ, 


BA, 


BB, 


BG, 


BR, 


BW, 


BY, 


BZ, 


CA, CH, 






CN, 


CO, 


CR, 


CU, 


CZ, 


DE, 


DK, 


DM, 


DZ, 


EC, 


EE, 


EG, 


ES, 


FI, 


GB, GD, 






GE, 


GH, 


GM, 


HR, 


HU, 


ID, 


IL, 


IN, 


IS, 


JP, 


KE, 


KG, 


KP, 


KR, 


KZ, LC, 






LK, 


LR, 


LS, 


LT, 


LU, 


LV, 


MA, 


MD, 


MG, 


MK, 


MN, 


MW, 


MX, 


MZ, 


NA, NI, 






NO, 


NZ, 


OM, 


PG, 


PH, 


PL, 


PT, 


RO, 


RU, 


SC, 


SD, 


SE, 


SG, 


SK, 


SL, SY, 






TJ, 


TM, 


TN, 


TR, 


TT, 


TZ, 


UA, 


UG, 


US, 


uz, 


VC, 


VN, 


YU, 


ZA, 


ZM, ZW 




RW: 


BW, 


GH, 


GM, 


KE, 


LS, 


MW, 


MZ, 


NA, 


SD, 


SL, 


sz. 


TZ, 


UG, 


ZM, 


ZW, AM, 






AZ, 


BY, 


KG, 


KZ, 


MD, 


RU, 


TJ, 


TM, 


AT, 


BE, 


BG, 


CH, 


CY, 


CZ, 


DE, DK, 






EE, 


ES, 


FI, 


FR, 


GB, 


GR, 


HU, 


IE, 


IT, 


LU, 


MC, 


NL, 


PL, 


PT, 


RO, SE, 






SI, 


SK, 


TR, 


BF, 


BJ, 


CF, 


CG, 


CI, 


CM, 


GA, 


GN, 


GQ, 


GW, 


ML, 


MR, NE, 






SN, 


TD, 


TG 


























KITY 


APPLN . 


INFO 














US 2003- 


502556P 




P 20030912 



GI 




AB The invention relates to a combination, particularly a synergistic 

combination, of an alpha-2-delta ligand and a dual serotonin-noradrenaline 
reuptake inhibitor (DSNRI) or one or both of a selective serotonin 
reuptake inhibitor (SSRI) and a selective noradrenaline reuptake inhibitor 
(SNRI), and pharmaceutically acceptable salts thereof, pharmaceutical 
compns. thereof and their use in the treatment of pain, particularly 
neuropathic pain (no biol . data). For instance, 3-amino-5-'methyloctanoic 
acid hydrochloride (I?HC1) was prepd. from (S) -citronellyl bromide in 
eight steps. 

IT 93413-62-8 / 0-Desmethylvenlaf axine 

RL: THU (Therapeutic use); BIOL (Biological study); USES (Uses) 

(dual serotonin-noradrenaline reuptake inhibitor; pharmaceutical 
combinations comprising alpha-2-delta ligands and dual 
serotonin-noradrenaline reuptake inhibitors) 

RN 93 413-62 - 8 HCAPLUS 



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11/22/05 



Page 17 of 51 



CN Phenol, 4- [2- (dimethyl ami no) -1- (1-hydroxycyclohexyl) ethyl] - {9CI) (CA 
INDEX NAME) 



Me 2N-CH2 




CH ^ 



0H-: 



::HQ: 



L4 ANSWER 11 OF 38 HCAPLUS COPYRIGHT 2005 ACS on STN 



ACCESSION NUMBER 
DOCUMENT NUMBER: 
TITLE: 



AUTHOR (S) 



CORPORATE SOURCE: 



SOURCE 



PUBLISHER: 
DOCUMENT TYPE 
LANGUAGE : 
AB 



IT 



RN 
CN 



2005 : 105997 HCAPLUS 
142:328916 

QSAR treatment of drugs transfer into human breast 
milk 

Katritzky, Alan R.; Dobchev, Dimitar A. ; Huer, Evrim; 
Fara, Dan C; Karelson, Mati 

Center for Heterocyclic Compounds, Department of 
Chemistry, University of Florida, Gainesville, FL, 
32611, USA 

Bioorganic & Medicinal Chemistry (2005), 13(5), 
1623-1632 

CODEN: BMECEP; ISSN: 0968-0896 
Elsevier Ltd. 
Journal 
English 

A satisfactory model is developed using for the correlation and prediction 
of milk to plasma concn. ratios (M/P ratio) for diverse pharmaceuticals. 
A set of exptl . derived M/P ratio values were collected from the 
literature for 115 widely used pharmaceuticals. The exptl. logarithmic 
M/P ratios were tested with more than 850 theor. mol. descriptors 
including constitutional, topol . , geometrical, quantum chem. , thermodn., 
and electrostatic types. Based on the data set, for 100 commonly used 
drugs, a seven-parameter QSAR model was derived that shows a satisfactory 
(R2 = 0.791) correlation between predicted and obsd. values of log (M/P) 
ratio . 

93413-62-8 / 0-Desmethylvenlaf axine 

RL: PAC (Pharmacological activity); PRP (Properties); THU 
(Therapeutic use); BIOL (Biological study); USES (Uses) 

(QSAR treatment of drug transfer into human breast milk) 
93413-62-8 HCAPLUS 

Phenol, 4- [2- (dimethylamino) -1- (1-hydroxycyclohexyl) ethyl] - (9CI) (CA 
INDEX NTUffi) 



OH 



:H0; 



REFERENCE COUNT: 



126 THERE ARE 126 CITED REFERENCES AVAILABLE FOR 

THIS RECORD. ALL CITATIONS AVAILABLE IN THE RE 

FORMAT 



L4 ANSWER 12 OF 38 



HCAPLUS COPYRIGHT 2005 ACS on STN 



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Page 18 of 51 



ACCESSION NUMBER: 
DOCUMENT NUMBER: 
TITLE: 



AUTHOR (S) : 



CORPORATE SOURCE: 



SOURCE : 



PUBLISHER: 
DOCUMENT TYPE 

LANGUAGE : 
AB 



2005:68165 HCAPLUS 
143:19763 

Combination therapy with venlafaxine and carbamazepine 
in depressive patients not responding to venlafaxine: 
pharmacokinetic and clinical aspects 
Ciusani, Elio; Zullino, Daniele F.; Eap^ Chin B.; 
Brawand-Amey, Marlyse; Brocard, Murielle; Baumann, 
Pierre 

Unite de Biochimie et Psychopharmacologie Clinique, 
Departement Universitaire de Psychiatrie Adulte, 
Prilly-Lausanne, Switz . 

Journal of Psychopharmacology (London, United Kingdom) 
(2004), 18(4), 559-566 
CODEN: JOPSEQ; ISSN: 0269-8811 
Sage Publications Ltd. 
Journal 
English 

The chiral antidepressant venlafaxine (VEN) is both a serotonin and a 
norepinephrine uptake inhibitor. CYP2D6 and CYP3A4 contribute to its 
metab., which has been shown to be stereoselective. Ten CYP2D6 genotyped 
and depressive (F32x and F33x, ICD-10) patients participated in an open 
study on the pharmacokinetic and pharmacodynamic consequences of a 
carbamazepine augmentation in VEN non-responders . After an initial 4-wk 
treatment with VEN (195 ? 52 mg/day) , the only poor metabolizer out of 
10 depressive patients had the highest plasma concns . of S-VEN and R-VEN, 
resp., whereas those of R-O-dimethyl-VEN were lowest. Five non-responders 
completed the second 4-wk study period, during which they were submitted 
to a combined VEN-carbamazepine treatment. In the only non-responder to 
this combined treatment, there was a dramatic decrease of both enantiomers 
of VEN, 0-dimethylvenlaf axine, N-desmethyl venlafaxine and 
N, O-didesmethylvenlaf axine in plasma, which suggests non-compliance, 
although metabolic induction by carbamazepine cannot entirely be excluded. 
The administration of carbamazepine [mean ? SD, range: 360 ? 89 
(200-400) mg/day] over 4 wk did not result in a significant modification 
of the plasma concns. of the enantiomers of VEN and its O- and 
N-demethylated metabolites in the other patients. In conclusion, these 
preliminary observations suggest that the combination of VEN and 
carbamazepine represents an interesting augmentation strategy by its 
efficacy, tolerance and absence of pharmacokinetic modifications. 
However, these findings should be verified in a more comprehensive study. 
IT 93413-62-8 , 0-Desmethylvenlaf axine 

RL: PAC (Pharmacological activity); PKT (Pharmacokinetics); THU 
(Therapeutic use); BIOL (Biological study); USES (Uses) 

(pharmacokinetics showed that carbamazepine did not significantly 
change plasma concn. of venlafaxine enantiomer R-VEN and S-VEN in 
depressive patient not responding to VEN) 
RN 93413-62-8 HCAPLUS 

CN Phenol, 4- [2- (dimethyl amino) -1- ( 1-hydroxycyclohexyl ) ethyl] - (9CI) (CA 
INDEX NAME) 




REFERENCE COUNT: 47 THERE ARE 47 CITED REFERENCES AVAILABLE FOR THIS 

RECORD. ALL CITATIONS AVAILABLE IN THE RE FORMAT 



http://stnweb.cas.org/cgi-bin/sdcgi?Sro=66588-0991124355-200&APP=stnweb& 



11/22/05 



Page 19 of 51 



L4 ANSWER 13 OF 38 HCAPLUS COPYRIGHT 2005 ACS on STN 



2004 : 1035019 HCAPLUS 
142:11574 

Therapeutic compositions including resin-loaded 
bioavailability enhancers 
Hughes, Lyn 

Rohm and Haas Company, USA 

Eur. Pat. Appl., 10 pp. 

CODEN: EPXXDW 

Patent 

English 

1 



KIND DATE APPLICATION NO. DATE 



Al 20041201 EP 2004-252933 20040518 

R: AT, BE, CH, DE, DK, ES, FR, GB, GR, IT, LI, LU, NL, SE, MC, PT, 

IE, SI, LT, LV, FI, RO, MK, CY, AL, TR, BG, CZ, EE, HU, PL, SK, HR 
JP 2004359665 A2 20041224 JP 2004-29032 20040205 



US 2004241135 


Al 


20041202 


US 


2004- 


854906 


20040527 


PRIORITY APPLN. INFO.: 






US 


2003- 


474663P 


P 20030530 



PlB The present invention relates to a resin comprising a bio-enhancer and an 
optional therapeutically active ingredient or precursor thereof loaded 
thereon. The bio-enhancer is ionizable or non-ionizable, and the resin 
may be a cation exchange resin or an anion exchange resin. For example, 
resin loaded with both active ingredient and bioenhancers was produced by 
mixing 0-desmethylvenlaf axine with strongly basic anion exchange resin 
ethanol solns., followed by adding succinic acid and then filtered and 
dried to obtain the resinate contg. 0-desmethylvenlaf axine succinate. 

IT 93413-62-8 , o-Desmethyl venlafaxine 

RL: PEP (Physical, engineering or chemical process); PYP (Physical 
process); RCT (Reactant); THU (Therapeutic use) ; BIOL 
(Biological study); PROC (Process); RACT (Reactant or reagent); USES 
(Uses) 

(therapeutic compns. contg. resin-loaded bioavailability enhancers and 

therapeutic agents) 
RN 93413-62-8 HCAPLUS 

CN Phenol, 4- [2- (dimethylamino) -1- (1-hydroxycyclohexyl) ethyl] - (9CI) (CA 
INDEX NAME) 




IT 448904'47-O P 

RL: PEP (Physical, engineering or chemical process); PYP (Physical 
process); SPN (Synthetic preparation); THU (Therapeutic use); 
BIOL (Biological study); PREP (Preparation); PROC (Process); USES (Uses) 
(therapeutic compns. contg. resin-loaded bioavailability enhancers and 
therapeutic agents) 
RN 448904-47-0 HCAPLUS 

CN Butanedioic acid, compd. with 4- [2- (dimethylamino) -1- ( 1- 

hydroxycyclohexyl) ethyl] phenol (1:1) (9CI) (CA INDEX NAME) 

CM 1 



ACCESSION NUMBER: 
DOCUMENT NUMBER: 
TITLE: 

INVENTOR (S) : 
PATENT ASSIGNEE (S) : 
SOURCE : 

DOCUMENT TYPE: 
LANGUAGE : 

FAMILY ACC. NUM. COUNT: 
PATENT INFORMATION: 

PATENT NO. 

EP 1481690 



http://stnwebxas.org/cgi-bin/sdcgi?SID=66588-0991124355-200&APP=stoweb& 



11/22/05 



Page 20 of 51 



CRN 93413-62-8 
CMF C16 H25 N 02 



Me2N-CH2 




OH 



CM 2 

CRN 110-15-6 
CMF C4 H6 04 



REFERENCE COUNT: 



THERE ARE 3 CITED REFERENCES AVAILABLE FOR THIS 
RECORD. ALL CITATIONS AVAILABLE IN THE RE FORMAT 



ANSWER 14 OF 38 HCAPLUS COPYRIGHT 2005 ACS on STN 



HCAPLUS 




ACCESSION NUMBER 
DOCUMENT NUMBER: 
TITLE: 



AUTHOR (S) 



CORPORATE SOURCE: 



SOURCE 



PUBLISHER: 
DOCUMENT TYPE 
LANGUAGE : 
AB 



2004:635508 
142:69012 

A pilot study of newer antidepressant concentrations 
in cord and maternal serum and possible effects in the 
neonate 

Rampono, Jonathan; Proud, Stephen; Hackett, L. Peter; 
Kristensen, Judith H.; Ilett, Kenneth F. 
Department of Psychological Medicine, Women's and 
Children's Health Service Subiaco, Subiaco, 6008, 
Australia 

International Journal of Neuropsychopharmacology 
(2004), 7(3), 329-334 
CODEN: IJNUFB; ISSN: 1461-1457 
Cambridge University Press 
Journal 
English 

Antidepressants are often used antenatally, and placental transfer may 
lead to adverse effects (toxicity) in the neonate. Pregnant women taking 
fluoxetine (n=4) , sertraline (n=4), paroxetine (n=2) or venlafaxine (n=l) 
in the last trimester were studied. Maternal and cord sera were collected 
at delivery and infant serum on day 5 after birth for measurement of 
antidepressant concns . Neonatal Abstinence Scores (NAS) were measured in 
the infants on days 1-3 after birth. In maternal serum, median drug 
concns. were: fluoxetine (96 ng/1) , norf luoxetine (110 |ig/l) , 
sertraline (11 ^ig/l) , desmethylsertraline (38 ng/1), paroxetine 
(mean 12 ^ig/1) , venlafaxine (220 ^g/1), and 0-desmethyl venlafaxine 
(392 ng/1) . Corresponding median values in cord serum were: fluoxetine 
(65 ng/1), norfluoxetine (81 ^ig/l), sertraline (10 |ig/l) , 
desmethylsertraline (27 ^g/1), paroxetine (mean 6 jig/l) , venlafaxine 
(232 \ig/l) , and O-desmethyl venlafaxine (406 \ig/l) , Corresponding 
median cord: maternal concn. ratios were 0.67 for fluoxetine and 0.72 for 
norfluoxetine, 0.67 for sertraline and 0.63 for demethylsertraline, 0.52 
(mean) for paroxetine, and 1.1 and 1.0 for venlafaxine and 
O-desmethyl venlafaxine resp. The neonates of two patients taking 



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Page 21 of 51 



fluoxetine had high NAS. Only fluoxetine and norf luoxetine were detected 
in infant serum. Our data show substantial placental transfer of 
antidepressants, but only fluoxetine persisted in the infant's serum. 
Neonatal toxicity may be assocd. with serotonin uptake blockade, and also 
be influenced by neonatal clearance. 
IT 93413-62-8 , 0-Desmethylvenlaf axine 

RL: ADV (Adverse effect, including toxicity); PAC (Pharmacological 
activity) ; THU (Therapeutic use) ; BIOL (Biological study) ; USES 
(Uses) 

(antidepressant infusion showed effective substantial placental 
transfer of methylvenlafaxine, showed no persistence in infant serum 
leading to neonatal toxicity indicating assocn. of serotonin re-uptake 

blockade and neonatal clearance) 
RN 93413-62-8 HCAPLUS 

CN Phenol, 4- [2- (dimethyl ami no) -1- ( 1-hydroxycyclohexyl) ethyl] - (9CI) (CA 
INDEX NAME) 



Me 2N-CH2 



HO 




OH 



REFERENCE COUNT: 



38 THERE ARE 38 CITED REFERENCES AVAILABLE FOR THIS 
RECORD. ALL CITATIONS AVAILABLE IN THE RE FORMAT 




ANSWER 15 OF 38 



ACCESSION NUMBER: 
DOCUMENT NUMBER: 
TITLE: 

INVENTOR (S) : 



PATENT ASSIGNEE (S) : 
SOURCE : 

DOCUMENT TYPE: 
LANGUAGE : 

FAMILY ACC. NUM. COUNT: 
PATENT INFORMATION: 



HCAPLUS COPYRIGHT 2005 ACS on STN 



2004:354797 HCAPLUS 
140:350606 

Use of norepinephrine reuptake modulators for 

preventing and treating vasomotor symptoms 

Deecher, Darlene Coleman; Merchenthaler, Istvan 

Joseph; Leventhal, Liza; Sipe, Kimberly Jean; 

O'Connor, Lawrence Thomas 

Wyeth, John, and Brother Ltd., USA 

PCT Int. Appl., 65 pp. 

CODEN: PIXXD2 

Patent 

English 

3 



PATENT NO. KIND DATE 



WO 


2004035058 




Al 




20040429 




W: 


AE, 


AG, 


AL, 


AM, 


AT, 


AU, 


AZ, 






CO, 


CR, 


CU, 


CZ, 


DE, 


DK, 


DM, 






GH, 


GM, 


HR, 


HU, 


ID, 


IL, 


IN, 






LR, 


LS, 


LT, 


LU, 


LV, 


MA, 


MD, 






PG, 


PH, 


PL, 


PT, 


RO, 


RU, 


SC, 






TR, 


TT, 


TZ, 


UA, 


UG, 


US, 


uz. 




RW: 


GH, 


GM, 


KE, 


LS, 


MW, 


MZ, 


SD, 






KG, 


KZ, 


MD, 


RU, 


TJ, 


TM, 


AT, 






FI, 


FR, 


GB, 


GR, 


HU, 


IE, 


IT, 






BF, 


BJ, 


CF, 


CG, 


CI, 


CM, 


GA, 


US 


2004152710 




Al 




20040805 


CA 


2502032 






AA 




20040429 


EP 


1551413 






Al 




20050713 



APPLICATION NO. ■ DATE 



WO 20Q3-US32759 20031015 



BA, 


BB, 


BG, 


BR, 


BY, 


BZ, 


CA, 


CH, 


CN, 


DZ, 


EC, 


EE, 


EG, 


ES, 


FI, 


GB, 


GD, 


GE, 


IS, 


JP, 


KE, 


KG, 


KP, 


KR, 


KZ, 


LC, 


LK, 


MG, 


MK, 


MN, 


MW, 


MX, 


MZ, 


NO, 


NZ, 


OM, 


SD, 


SE, 


SG, 


SK, 


SL, 


SY, 


TJ, 


TM, 


TN, 


VC, 


VN, 


YU, 


ZA, 


ZM, 


zw 








SL, 


SZ, 


TZ, 


UG, 


ZM, 


zw. 


AM, 


AZ, 


BY, 


BE, 


BG, 


CH, 


CY, 


CZ, 


DE, 


DK, 


EE, 


ES, 


LU, 


MC, 


NL, 


PT, 


RO, 


SE, 


SI, 


SK, 


TR, 


GN, 


GQ, 


GW, 


ML, 


MR, 


NE, 


SN, 


TD, 


TG 



US 2003-685812 20031014 
CA 2003-2502032 20031015 
EP 2003-774853 20031015 



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11/22/05 



Page 22 of 51 





R: 


AT, 


BE, 


CH, 


DE, 


DK, 


ES, 


FR, 


GB, 


GR, 


IT, 


LI, 


LU, 


NL, 


SE, 


MC, PT, 






IE, 


SI, 


LT, 


LV, 


FI, 


RO, 


MK, 


CY, 


AL, 


TR, 


BG, 


CZ, 


EE, 


HU, 


SK 


BR 


2003015355 




A 




20050823 




BR 2003- 


15355 




20031015 


US 


2005130987 




Al 




20050616 




US 2004- 


962897 




20041012 


WO 


2005037260 




A2 




20050428 




WO 2004- 


US33754 




20041013 




W: 


AE, 


AG, 


AL, 


AM, 


AT, 


AU, 


AZ, 


BA, 


BB, 


BG, 


BR, 


BW, 


BY, 


BZ, 


CA, CH, 






CN/ 


CO, 


CR, 


CU, 


CZ, 


DE, 


DK, 


DM, 


DZ, 


EC, 


EE, 


EG, 


ES, 


FI, 


GB, GD, 






GE, 


GH, 


GM, 


HR, 


HU, 


ID, 


IL, 


IN, 


IS, 


JP, 


KE, 


KG, 


KP, 


KR, 


KZ, LC, 






LK, 


LR, 


LS, 


LT, 


LU, 


LV, 


MA, 


MD, 


MG, 


MK, 


MN, 


MW, 


MX, 


MZ, 


NA, NI, 






NO, 


NZ, 


OM, 


PG, 


PH, 


PL, 


PT, 


RO, 


RU, 


SC, 


SD, 


SE, 


SG, 


SK, 


SL, SY, 






TJ, 


TM, 


TN, 


TR, 


TT, 


TZ, 


UA, 


UG, 


US, 


UZ, 


VC, 


VN, 


YU, 


ZA, 


ZM, ZW 




RW: 


BW, 


GH, 


GM, 


KE, 


LS, 


MW, 


MZ, 


NA, 


SD, 


SL, 


SZ, 


TZ, 


UG, 


ZM, 


ZW, AM, 






AZ, 


BY, 


KG, 


KZ, 


MD, 


RU, 


TJ, 


TM, 


AT, 


BE, 


BG, 


CH, 


CY, 


CZ, 


DE, DK, 






EE, 


ES, 


FI, 


FR, 


GB, 


GR, 


HU, 


IE, 


IT, 


LU, 


MC, 


NL, 


PL, 


PT, 


RO, SE, 






SI, 


SK, 


TR, 


BF, 


BJ, 


CF, 


CG, 


CI, 


CM, 


GA, 


GN, 


GQ, 


GW, 


ML, 


MR, NE, 






SN, 


TD, 


TG 


























PRIORITY APPLN. 


INFO 














US 2002- 


418591P 




P 20021015 






















US 2003- 


6858 


12 




A 20031014 






















US 2003- 


5108 


97P 




P 20031014 






















WO 2003- 


US32759 




W 20031015 






















US 2004- 


962897 




A 20041012 



AB The invention discloses the use of compds. and compn. of compds. that 
modulate norepinephrine levels for the prevention and treatment of 
vasomotor symptoms, such as hot flush, caused by, inter alia, 
thermoregulatory dysfunctions. Compds. of the invention include e.g. 
desipramine . 

IT 93413-62-8 , DVS 233 142761-11-3 142761-12-4 

RL: PAC (Pharmacological activity); THU (Therapeutic use); BIOL 
(Biological study) ; USES (Uses) 

(norepinephrine reuptake modulators for preventing and treating 
vasomotor symptoms) 

RN 93413-62-8 HCAPLUS 

CN Phenol, 4- [2- (dimethylamino) -1- (1-hydroxycyclohexyl) ethyl] - {9CI) (CA 
INDEX NAME) 




RN 142761-11-3 HCAPLUS 

CN Phenol, 4-[ (IR) -2- (dimethylamino) -1- (1-hydroxycyclohexyl) ethyl] - (9CI) 
(CA INDEX NAME) 

Absolute stereochemistry. Rotation (-) . 




RN 142761-12-4 HCAPLUS 

CN Phenol, 4- [ (IS) -2- (dimethylamino) -1- (1-hydroxycyclohexyl) ethyl] - (9CI) 
(CA INDEX NAME) 

Absolute stereochemistry. Rotation {+) . 



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Page 23 of 51 




REFERENCE COUNT: 5 THERE ARE 5 CITED REFERENCES AVAILABLE FOR THIS 

RECORD. ALL CITATIONS AVAILABLE IN THE RE FORMAT 



L4 



ANSWER 16 OF 38 HCAPLUS COPYRIGHT 2005 ACS on STN 



Full 






Text 







ACCESSION NUMBER: 
DOCUMENT NUMBER: 
TITLE: 



INVENTOR (S) : 
PATENT ASSIGNEE (S) : 
SOURCE : 

DOCUMENT TYPE: 
L7\NGUAGE : 

FAMILY ACC. NUM. COUNT: 
PATENT INFORMATION: 



2004 : 354778 HCAPLUS 
140:350603 

A method of treating vasomotor symptoms using a 

compound having norepinephrine reuptake inhibitor 

activity and 5-HT2a antagonistic activity 

Deecher, Darlene Coleman; Merchenthaler, Istvan Joseph 

Wyeth, John, and Brother Ltd., USA 

PCT Int. Appl., 34 pp. 

CODEN: PIXXD2 

Patent 

English 

1 



PATENT NO. KIND DATE APPLICATION NO. DATE 



WO 


2004035036 




Al 




20040429 




WO 2003- 


US32554 




20031015 




W: 


AE, 


AG, 


AL, 


AM, 


AT, 


AU, 


AZ, 


BA, 


BB, 


BG, 


BR, 


BY, 


BZ, 


CA, 


CH, 


CN, 






CO, 


CR, 


CU, 


CZ, 


DE, 


DK, 


DM, 


DZ, 


EC, 


EE, 


EG, 


ES, 


FI, 


GB, 


GD, 


GE, 






GH, 


GM, 


HR, 


HU, 


ID, 


IL, 


IN, 


IS, 


JP, 


KE, 


KG, 


KP, 


KR, 


KZ, 


LC, 


LK, 






LR, 


LS, 


LT, 


LU, 


LV, 


MA, 


MD, 


MG, 


MK, 


MN, 


MW, 


MX, 


MZ, 


NO, 


NZ, 


OM, 






PG, 


PH, 


PL, 


PT, 


RO, 


RU, 


SC, 


SD, 


SE, 


SG, 


SK, 


SL, 


SY, 


TJ, 


TM, 


TN, 






TR, 


TT, 


TZ, 


UA, 


UG, 


US, 


UZ, 


vc. 


VN, 


YU, 


ZA, 


ZM, 


ZW 










RW: 


GH, 


GM, 


KE, 


LS, 


MW, 


MZ, 


SD, 


SL, 


SZ, 


TZ, 


UG, 


ZM, 


zw. 


AM, 


AZ, 


BY, 






KG, 


KZ, 


MD, 


RU, 


TJ, 


TM, 


AT, 


BE, 


BG, 


CH, 


CY, 


CZ, 


DE, 


DK, 


EE, 


ES, 






FI, 


FR, 


GB, 


GR, 


HU, 


IE, 


IT, 


LU, 


MC, 


NL, 


PT, 


RO, 


SE, 


SI, 


SK, 


TR, 






BF, 


BJ, 


CF, 


CG, 


CI, 


CM, 


GA, 


GN, 


GQ, 


GW, 


ML, 


MR, 


NE, 


SN, 


TD, 


TG 


US 


2004180879 




Al 




20040916 




US 2003- 


685974 




20031014 


CA 


2502027 






AA 




20040429 




CA 2003- 


2502027 




20031015 


EP 


1551380 






Al 




20050713 




EP 2003- 


774828 




20031015 




R: 


AT, 


BE, 


CH, 


DE, 


DK, 


ES, 


FR, 


GB, 


GR, 


IT, 


LI, 


LU, 


NL, 


SE, 


MC, 


PT, 






IE, 


SI, 


LT, 


LV, 


FI, 


RO, 


MK, 


CY, 


AL, 


TR, 


BG, 


CZ, 


EE, 


HU, 


SK 




BR 


2003015346 




A 




20050823 




BR 2003- 


15346 




20031015 


PRIORITY 


APPLN . 


INFO 














US 2002- 


418516P 




P 20021015 






















US 2003- 


685974 




A 20031014 






















WO 2003- 


US32554 




W 20031015 



AB The invention discloses the use of compds. and compns. of compds. that 
modulate norepinephrine levels for the treatment of vasomotor symptoms, 
e.g. thermoregulatory disorders. The invention also discloses the use of 
compds, and compns. of compds. having norepinephrine reuptake inhibitor 
(NRI) activity alone or norepinephrine reuptake inhibitor and serotonin 
reuptake inhibitor (NRI/SRI) dual activity in combination with 5-HT2a 
receptor antagonist activity. 

IT 93413-62-8 , Desvenlaf axine 

RL: PAC (Pharmacological activity); THU (Therapeutic use); BIOL 
(Biological study); USES (Uses) 



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11/22/05 



Page 24 of 51 



(compds. with norepinephrine reuptake inhibitor activity and 5-HT2a 
antagonistic activity for treatment of vasomotor symptoms) 
RN 93413-62-8 HCAPLUS 

CN Phenol, 4- [2- (dimethylamino) -1- (1-hydroxycyclohexyl) ethyl] - (9CI) (CA 
INDEX NAME) 




REFERENCE COUNT: ' 6 THERE ARE 6 CITED REFERENCES AVAILABLE FOR THIS 

RECORD. ALL CITATIONS AVAILABLE IN THE RE FORMAT 

L4 ANSWER 17 OF 38 HCAPLUS COPYRIGHT 2005 ACS on STN 




ACCESSION NUMBER: 
DOCUMENT NUMBER: 
TITLE: 



INVENTOR (S) : 



PATENT ASSIGNEE (S) : 
SOURCE : 

DOCUMENT TYPE: 
LANGUAGE : 

FAMILY ACC. NUM. COUNT: 
PATENT INFORMATION: 



2004 : 354777 HCAPLUS 
140:350602 

Use of norepinephrine reuptake modulators for 

preventing and treating vasomotor symptoms 

Deecher, Darlene Coleman; Merchenthaler, Istvan 

Joseph; Leventhal, Liza; Sipe, Kimberly Jean; 

O'Connor, Lawrence Thomas 

Wyeth, John^ and Brother Ltd., USA 

PCT Int. Appl., 58 pp. 

CODEN: PIXXD2 

Patent 

English 

3 



PATENT NO. KIND DATE APPLICATION NO. DATE 



WO 


2004035035 




Al 




20040429 




WO 2003- 


US332760 




20031015 




W: 


AE, 


AG, 


AL, 


AM, 


AT, 


AU, 


AZ, 


BA, 


BB, 


BG, 


BR, 


BY, 


BZ, 


CA, 


CH, 


CN, 






CO, 


CR, 


CU, 


CZ, 


DE, 


DK, 


DM, 


DZ, 


EC, 


EE, 


EG, 


ES, 


FI, 


GB, 


GD, 


GE, 






GH, 


GM, 


HR, 


HU, 


ID, 


IL, 


IN, 


IS, 


JP, 


KE, 


KG, 


KP, 


KR, 


KZ, 


LC, 


LK, 






LR, 


LS, 


LT, 


LU, 


LV, 


MA, 


MD, 


MG, 


MK, 


MN, 


MW, 


MX, 


MZ, 


NI, 


NO, 


NZ, 






OM, 


PG, 


PH, 


PL, 


PT, 


RO, 


RU, 


SC, 


SD, 


SE, 


SG, 


SK, 


SL, 


SY, 


TJ, 


TM, 






TN, 


TR, 


TT, 


TZ, 


UA, 


UG, 


US, 


uz. 


VC, 


VN, 


YU, 


ZA, 


ZM, 


ZW 








RW: 


GH, 


GM, 


KE, 


LS, 


MW, 


MZ, 


SD, 


SL, 


sz. 


TZ, 


UG, 


ZM, 


zw, 


AM, 


AZ, 


BY, 






KG, 


KZ, 


MD, 


RU, 


TJ, 


TM, 


AT, 


BE, 


BG, 


CH, 


CY, 


CZ, 


DE, 


DK, 


EE, 


ES, 






FI, 


FR, 


GB, 


GR, 


HU, 


IE, 


IT, 


LU, 


MC, 


NL, 


PT, 


RO, 


SE, 


SI, 


SK, 


TR, 






BF, 


BJ, 


CF, 


CG, 


CI, 


CM, 


GA, 


GN, 


GQ, 


GW, 


ML, 


MR, 


NE, 


SN, 


TD, 


TG 


US 


2004143008 




Al 




20040722 




US 2003- 


684777 




20031014 


CA 


2502021 






AA 




20040429 




CA 2003- 


2502021 




20031015 


EP 


1551379 






Al 




20050713 




EP 2003- 


774854 




20031015 




R: 


AT, 


BE, 


CH, 


DE, 


DK, 


ES, 


FR, 


GB, 


GR, 


IT, 


LI, 


LU, 


NL, 


SE, 


MC, 


PT, 






IE, 


SI, 


LT, 


LV, 


FI, 


RO, 


MK, 


CY, 


AL, 


TR, 


BG, 


CZ, 


EE, 


HU, 


SK 




BR 


2003015314 




A 




20050816 




BR 2003- 


15314 




20031015 



PRIORITY APPLN. INFO,: US 2002-418591P P 20021015 

US 2003-684777 A 20031014 

WO 2003-US32760 W 20031015 

AB The invention discloses the use of compds. and compns. of compds. that 
modulate norepinephrine levels for the prevention and treatment of 
vasomotor symptoms, e.g. hot flush, caused by, inter alia, 
thermoregulatory dysfunctions. Compds. of the invention include e.g. 
venlaf axine. 



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11/22/05 



Page 25 of 51 



IT 93413-62-8 . DVS 233 142761-11-3 142761-12-4 

RL: PAC (Pharmacological activity); THU (Therapeutic use); BIOL 
(Biological study); USES (Uses) 

(norepinephrine reuptake modulators for preventing and treating 

vasomotor symptoms) 
RN 93413-62-8 HCAPLUS 

CN Phenol, 4- [2- ( dime thylamino) -1- ( 1-hydroxycyclohexyl ) ethyl] - (9CI) (CA 
INDEX NAME) 



Me2N"CH2 



HO 



OH 



RN 142761-11-3 
CN 



HCAPLUS 



Phenol, 4- [ (IR) -2- (dimethylamino) -1- (1-hydroxycyclohexyl) ethyl] - (9CI) 
(CA INDEX NAME) 



Absolute stereochemistry. Rotation (-) , 




RN 142761-12-4 HCAPLUS 

CN Phenol, 4- [ (IS) -2- (dimethylamino) -1- (1-hydroxycyclohexyl) ethyl] - (9CI) 
(CA INDEX NAME) 

Absolute stereochemistry. Rotation (+) . 




REFERENCE COUNT: 7 THERE ARE 7 CITED REFERENCES AVAILABLE FOR THIS 

RECORD. ALL CITATIONS AVAILABLE IN THE RE FORMAT 



ANSWER 18 OF 38 HCAPLUS COPYRIGHT 2005 ACS on STN 




ACCESSION NUMBER: 
DOCUMENT NUMBER: 
TITLE: 



INVENTOR (S) : 

PATENT ASSIGNEE (S): 
SOURCE : 

DOCUMENT TYPE: 
L7\NGUAGE : 



2004 : 181965 HCAPLUS 
140:205161 

Pharmaceutical preparations comprising a 5HT uptake 
inhibitor and a homopolymer or copolymer of 
N-vinylpyrrolidone 

Kankan, Rajendra Narayanrao; Rao, Dharmaraj 

Ramachandra 

Cipla Limited, India 

Brit. UK Pat. Appl., 13 pp. 

CODEN: BAXXDU 

Patent 

English 



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11/22/05 



Page 26 of 51 



FAMILY ACC. NUM. COUNT: 1 
PATENT INFORMATION: 

PATENT NO. KIND DATE APPLICATION NO. DATE 



GB 2392385 Al 20040303 GB 2002-20334 20020902 

PRIORITY APPLN. INFO.: GB 2002-20334 20020902 

AB Pharmaceutically acceptable prepns. are described comprising one or more 

5HT uptake inhibitors with an excipient matrix comprising a homopolymer or 
copolymer of N-vinylpyrrolidone in which the 5HT uptake inhibitors are 
complexed with the homopolymer or copolymer. The 5HT uptake inhibitors 
are preferably in amorphous form and may be selected from citalopram, 
venlafaxine, desmethyl venlafaxine, sertraline, fluoxetine and their 
salts. The homopolymer or copolymer is preferably a polyvinylpyrrolidone 
or crospovidone . The prepns. are suitable for the treatment of a range of 
diseases which are prevented, ameliorated or eliminated by the 
administration of a 5HT uptake inhibitor. Such diseases include 
depression, substance abuse and senile dementia. One or more 5HT uptake 
inhibitors together with a homopolymer or copolymer of N-vinylpyrrolidone 
may be used in the treatment of such diseases. For example, to a soln. of 
25 g of citalopram in 125 mL of ethanol was added 75 g of 
polyvinylpyrrolidone K30 at room temp, to obtain a clear soln. The soln. 
was coned, under vacuum at a temp, below 40? to give an amorphous 
solid, which was filtered off. The amt. of citalopram in the complex was 
22% to 28%. 
IT 93413--62-8 , 0-Desmethylvenlaf axine 

RL: THU (Therapeutic use); BIOL (Biological study); USES (Uses) 
(solid oral compns . comprising 5HT uptake inhibitor and 
vinylpyrrolidone polymer) 
RN 93413-62-8 HCAPLUS 

CN Phenol, 4- [2- (dimethyl amino) -1- ( 1-hydroxycyclohexyl) ethyl] - (9CI) (CA 



7 THERE ARE 7 CITED REFERENCES AVAILABLE FOR THIS 

RECORD. ALL CITATIONS AVAILABLE IN THE RE FORMAT 

HCAPLUS COPYRIGHT 2005 ACS on STN 



2003 : 931155 HCAPLUS 
139:391365 

Methods of treating gastrointestinal and genitourinary 
pain disorders using venlafaxine and derivatives 
Karlstadt, Robyn Gail; Lynn, Richard Brian; Burton, 
Michael Scott; Danilewitz, Mervyn 
Wyeth, John, and Brother Ltd., USA 
PCT Int. Appl., 17 pp. 
CODEN: PIXXD2 
Patent 
English 
FAMILY ACC. NUM. COUNT: 1 
PATENT INFORMATION: 

PATENT NO. KIND DATE APPLICATION NO. DATE 



INDEX NAME) 




REFERENCE COUNT: 



L4 ANSWER 19 OF 38 









1 'J 1 1 

Text 




^?nca5 1 



ACCESSION NUMBER: 
DOCUMENT NUMBER: 
TITLE: 



INVENTOR (S) : 

PATENT ASSIGNEE (S) : 
SOURCE : 

DOCUMENT TYPE: 
LANGUAGE : 



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11/22/05 



Page 27 of 51 



WO 


2003097029 




Al 




20031127 




WO 2003- 


US15230 




20030515 




W: AE, 


AG, 


AL, 


AM, 


AT, 


AU, 


AZ, 


BA, 


BB, BG, 


BR, 


BY, 


BZ, 


CA, CH, CN, 




CO, 


CR, 


CU, 


CZ, 


DE, 


DK, 


DM, 


DZ, 


EC, EE, 


ES, 


FI, 


GB, 


GD, GE, GH, 




GM, 


HR, 


HU, 


ID, 


IL, 


IN, 


IS, 


JP, 


KE, KG, 


KP, 


KR, 


KZ, 


LC, LK, LR, 




LS, 


LT, 


LU, 


LV, 


MA, 


MD, 


MG, 


MK, 


MN, MW, 


MX, 


MZ, 


NI, 


NO, NZ, OM, 




PH, 


PL, 


PT, 


RO, 


RU, 


SC, 


SD, 


SE, 


SG, SK, 


SL, 


TJ, 


TM, 


TN, TR, TT, 




TZ, 


UA, 


UG, 


US, 


UZ, 


VC, 


VN, 


YU, 


ZA, ZM, 


ZW 










RW: GH, 


GM, 


KE, 


LS, 


MW, 


MZ, 


SD, 


SL, 


SZ, TZ, 


UG, 


ZM, 


ZW, 


AM, AZ, BY, 




KG, 


KZ, 


MD, 


RU, 


TJ, 


TM, 


AT, 


BE, 


BG, CH, 


CY, 


CZ, 


DE, 


DK, EE- ES. 




FI, 


FR, 


GB, 


GR, 


HU, 


IE, 


IT, 


LU, 


MC, NL, 


PT, 


RO, 


SE, 


SI, SK, TR, 




BF, 


BJ, 


CF, 


CG, 


CI, 


CM, 


GA, 


GN, 


GQ, GW, 


ML, 


MR, 


NE, 


SN, TD, TG 


CA 


2485736 






AA 




20031127 




CA 2003- 


2485736 




20030515 


US 


2004019101 




Al 




20040129 




US 2003- 


438572 




20030515 


BR 


2003010083 




A 




20050215 




BR 2003- 


10083 




20030515 


EP 


1505960 






Al 




20050216 




EP 2003" 


753036 




20030515 




R: AT, 


BE, 


CH, 


DE, 


DK, 


ES, 


FR, 


GB, 


GR, IT, 


LI, 


LU, 


NL, 


SE, MC, PT, 




IE, 


SI, 


LT, 


LV, 


FI, 


RO, 


MK, 


CY, 


AL, TR, 


BG, 


CZ, 


EE, 


HU, SK 


JP 


2005530779 




T2 




20051013 




JP 2004- 


505028 




20030515 


^ITY APPLN. 


INFO. 














US 2002- 


381305P 




P 20020517 




















WO 2003- 


US15230 




W 20030515 



OTHER SOURCE(S): MARPAT 139:391365 

GI 




AB The invention provides a method of treating functional gastrointestinal 

and genitourinary disorders in a mammal by administering to the mammal an 
effective amt. of hydroxycycloalkane phenethylamine I where the dotted 
line represents optional unsatn.; Rl, R7 = H, alkyl; R2 = alkyl; R4 = H, 
alkyl, formyl, alkanol; R5, R6 = H, OH, alkyl, alkoxy, alkanoyloxy, cyano, 
nitro, alkylmercapto, amino, alkylamino, dialkylamino, alkanamido, halo, 
trifluoromethyl, or, taken together, methylenedioxy; n is [0-4], or a 
pharmaceutically acceptable salt thereof. 

IT 93413-62-8 , 0-DesmethylVenlaf axine 

RL: PAC (Pharmacological activity); THU (Therapeutic use); BIOL 
(Biological study); USES (Uses) 

(venlaf axine and derivs. for treatment of gastrointestinal and 
genitourinary pain disorders) 

RN 93413-62-8 HCAPLUS 

CN Phenol, 4- [2- (dimethyl ami no) -1- ( 1-hydroxycyclohexyl ) ethyl] - (9CI) (CA 
INDEX NAME) 



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11/22/05 



Page 28 of 51 



12 THERE ARE 12 CITED REFERENCES AVAIL7\BLE FOR THIS 
RECORD. ALL CITATIONS AVAILABLE IN THE RE FORMAT 

HCAPLUS COPYRIGHT 2005 ACS on STN 



2003:752480 HCAPLUS 
140:245936 

A High-Performance Liquid Chromatography Method with 
Photodiode-Array UV Detection for Therapeutic Drug 
Monitoring of the Nontricyclic Antidepressant Drugs 
Duverneuil, Charlotte; de la Grandmaison, Geoff roy 
Lorin; de Mazancourt, Philippe; Alvarez, Jean-Claude 
Laboratoire de Pharmacologie-Toxicologie and Service 
de Medecine Legale, Centre Hospitaller Universitaire 
Raymond Poincare, Garches, 92380, Fr. 
Therapeutic Drug Monitoring (2003), 25(5), 565-573 
CODEN: TDMODV; ISSN: 0163-4356 
Lippincott Williams & Wilkins 
Journal 
English 

AB A new rapid and sensitive high-performance liq. chromatog. method has been 
developed for the screening and detn. in human plasma of the 11 most 
commonly prescribed non-tricyclic antidepressants and two metabolites: 
fluoxetine, norf luoxetine, sertraline, paroxetine, citalopram, 
fluvoxamine, moclobemide, mirtazapine, milnacipram, toloxatone, 
venlafaxine, desmethyl venlafaxine, and viloxazine. It involves liq. -liq. 
extn. procedures followed by liq. chromatog. coupled to photodiode-array 
UV detection with three fixed wavelengths (220, 240, and 290 nm) . Compds. 
were sepd. on a 5-\m Hypurity C18 (ThermoHypersil ) analytic coliimn (250 
4.6 I mm i.d.) using a gradient of acetonitrile-phosphate buffer pH 
3.8 at a flow rate of 1.0 mL/min. The total anal, time was only 18 min 
per sample. Extn. recoveries were in the 74-109% range for 11 compds. but 
were of only 59% for moclobemide and less than 10% for toloxatone. 
Calibration curves were linear in the 25 to 1000 ng/mL range for all 
compds., all of them with coeffs. of detn. (r2 values) ? 0.999. 
Limits of detection (LCDs) ranged from 2.5 to 5 ng/mL except for 
toloxatone (10 ng/mL) . Intra-assay and inter-assay precision and accuracy 
were studied at two concn. levels (50 and 500 ng/mL) . The intra-assay 
coeffs. of variation (CVs) for all compds. were ? 7.6%, and all 
inter-assay CVs were below 11.5% except for milnacipram (14.8%). The 
intra-assay and inter-assay accuracies for all compds. were found to be 
within 88.4% and 105.9% at 50 ng/mL and within 87.2% and 100.5% at 500 
ng/mL. The performance of the method allows the therapeutic drug 
monitoring of the most prescribed non-tricyclic antidepressant drugs as 
well as its use in toxicol. screening. 

IT 93413-62-8 / 0-Desmethylvenlaf axine 

RL: ANT (Analyte) ; BSU (Biological study, unclassified); THU 
(Therapeutic use) ; ANST (Analytical study) ; BIOL (Biological study) ; 
USES (Uses) 

(metabolite; HPLC method with photodiode-array UV detection for 
therapeutic drug monitoring of the non-tricyclic antidepressant drugs) 
RN 93413-62-8 HCAPLUS 

CN Phenol, 4- [2- (dimethyl ami no) -1- (1-hydroxycyclohexyl) ethyl] - (9CI) (CA 



l1e2N-CH2 ^^-^ 
REFERENCE COUNT: 



L4 ANSWER 20 OF 38 



ACCESSION NUMBER: 
DOCUMENT NUMBER: 
TITLE: 



AUTHOR (S) : 
CORPORATE SOURCE: 

SOURCE : 

PUBLISHER: 
DOCUMENT TYPE: 

LANGUAGE : 



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Page 29 of 51 

INDEX NAME) 



HO-^ OH 

REFERENCE COUNT: 



21 THERE ARE 21 CITED REFERENCES AVAILABLE FOR THIS 
RECORD. ALL CITATIONS AVAILABLE IN THE RE FORMAT 



ANSWER 21 OF 38 HCAPLUS COPYRIGHT 2005 ACS on STN 



HCAPLUS 




ACCESSION NUMBER: 
DOCUMENT NUMBER: 
TITLE : 



AUTHOR (S) : 



CORPORATE SOURCE: 



SOURCE : 



PUBLISHER: 
DOCUMENT TYPE 
LANGUAGE : 
AB 



fast and reliable 

We therefore devised 



2003:584504 
140:172 

Analysis of eighteen antidepressants^ four atypical 

antipsychotics and active metabolites in serum by 
liquid chromatography: a simple tool for therapeutic 
drug monitoring 

Frahnert, Christine; Rao, Marie Luise; Grasmader, 

Katja 

Department of Psychiatry, University of Bonn, Bonn, 
D-53105, Germany 

Journal of Chromatography, B: Analytical Technologies 
in the Biomedical and Life Sciences (2003), 794(1), 
35-47 

CODEN: JCBAAI; ISSN: 1570-0232 
Elsevier Science B.V. 
Journal 
English 

Therapeutic drug monitoring necessitates efficient, 
anal, methods validated by external quality control 
an isocratic reversed-phase HPLC method with UV detection and optimized 
this to quantify mirtazapine, reboxetine, moclobemide, venlafaxine, 
0-desmethylvenlafaxine, paroxetine, fluvoxamine, fluoxetine, 
norf luoxetine, sertraline, citalopram, amitriptyline, nortriptyline, 
imipramine, desipramine, doxepin, nordoxepin, clomipramine, 
norclomipramine, trimipramine, mianserine, maprotiline, normaprotiline, 
amisulpride, clozapine, norclozapine, quetiapine, risperidone and 
9-OH- risperidone in human serum. After solid-phase extn. of the drugs and 
metabolites, the chromatog. sepn. was achieved on a Nucleosil 100-Protect 
1 column with acetonitrile-potassium dihydrogenphosphate buffer as mobile 
phase. The method was validated for therapeutic and toxic serum ranges. 
A linear relationship (r>0.998) was obtained between the concn. and the 
detector signal. Recoveries were between 75 and 99% for the drugs and 
metabolites. The accuracy of the quality control samples, expressed as 
percent recovery, ranged from 91 to 118%; intra- and inter-assay- relative 
std. deviations were 0.9-10.2% and 0.9-9.7%, resp. Addnl . external 
quality control is carried out since 3 yr. This method is applicable to 
rapidly and effectively analyze serum or plasma samples for therapeutic 
drug monitoring of about 30 antidepressants and atypical antipsychotics. 
IT 93413-62-8 ^ O-Desmethylvenlaf axine 

RL: ANT (Analyte) ; BSU (Biological study, unclassified); THU 
(Therapeutic use) ; ANST (Analytical study) ; BIOL (Biological study) ; 
USES (Uses) 

(anal, of antidepressants and atypical antipsychotics and active 
metabolites in serum by liq. chromatog. for therapeutic drug 
monitoring) ir 
RN 93413-62-8 HCAPLUS 



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CN Phenol, 4- [2- (dimethyl amino) -1- (1-hydroxycyclohexyl) ethyl] - (9CI) (CA 
INDEX NAME) 



39 THERE ARE 39 CITED REFERENCES AVAILABLE FOR THIS 
RECORD. ALL CITATIONS AVAILABLE IN THE RE FORMAT 

HCAPLUS COPYRIGHT 2005 ACS on STN 



2003:262485 HCAPLUS 
139:207091 

Inhibition of P-glycoprotein by newer antidepressants 
Weiss, Johanna; Dormann, Sven-Maria Gregor; 
Martin-Facklam, Meret; Kerpen, Christian Johannes; 
Ketabi-Kiyanvash, Nahal; Haefeli, Walter Emil 
Department of Internal Medicine VI, Clinical 
Pharmacology, and Pharmacoepidemiology, University of 
Heidelberg, Heidelberg, Germany 

Journal of Pharmacology and Experimental Therapeutics 
(2003), 305(1), 197-204 
CODEN: JPETAB; ISSN: 0022-3565 

American Society for Pharmacology and Experimental 
Therapeutics 
Journal 
English 

AB Pharmacokinetic drug-drug interactions often occur at the level of 

P-glycoprotein (Pgp) . To study possible interactions caused by the newer 
antidepressants we investigated citalopram, fluoxetine, fluvoxamine, 
paroxetine, reboxetine, sertraline, and venlafaxine and their major 
metabolites desmethylcitalopram, norf luoxetine, paroxetine-metabolite 
(paroxetine-M) , desmethylsertraline, N-desmethyl venlafaxine, and 
0-desmethylvenlaf axine for their ability to inhibit Pgp. Pgp inhibition 
was studied by a fluorometric assay using calcein-acetoxymethylester as 
Pgp substrate and two different cell systems: L-MDRl cells (model for 
human Pgp) and primary porcine brain capillary endothelial cells (pBCECs, 
model for the blood-brain barrier) . Both cell systems proved to be 
suitable for the evaluation of Pgp inhibitory potency of drugs. All 
antidepressants tested except O-desmethylvenlaf axine showed Pgp inhibitory 
activity with sertraline, desmethylsertraline, and paroxetine being the 
most potent, comparable with the well known Pgp inhibitor quinidine. In 
L^MDRl cells fluoxetine, norf luoxetine, fluvoxamine, reboxetine, and 
paroxetine-M revealed intermediate Pgp inhibition and citalopram, 
desmethylcitalopram, venlafaxine, and N-desmethylvenlaf axine were only 
weak inhibitors. The ranking order was similar in pBCECs. The fact that 
some of the compds. tested exert Pgp inhibitor effects at similar concns. 
as quinidine suggests that pharmacokinetic drug-drug interactions between 
the newer antidepressants and Pgp substrates should now be thoroughly 
studied in vivo. 

IT 93413-62-8 , 0-Desmethyl venlafaxine 

RL: ADV (Adverse effect, including toxicity); PAC (Pharmacological 
activity) ; XHU (Therapeutic use) ; BIOL (Biological study) ; USES 
(Uses) 

(antidepressant inhibition of P-glycoprotein in relation to 
pharmacokinetic drug interactions) 




REFERENCE COUNT: 



L4 ANSWER 22 OF 38 




ACCESSION NUMBER: 
DOCUMENT NUMBER: 
TITLE: 
AUTHOR (S) : 



CORPORATE SOURCE: 



SOURCE : 



PUBLISHER: 

DOCUMENT TYPE: 
LTU^GUAGE : 



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RN 93413-62-8 HCAPLUS 

CN Phenol, 4- [2- (dimethyl ami no) -1- ( 1-hydroxycyclohexyl) ethyl] - {9CI) 
INDEX NAME) 



(CA 



HO* 



Me2N^CH2 





OH 



REFERENCE COUNT: 



40 THERE ARE 40 CITED REFERENCES AVAILABLE FOR THIS 
RECORD. ALL CITATIONS AVAILABLE IN THE RE FORMAT 



L4 ANSWER 23 OF 38 HCAPLUS COPYRIGHT 2005 ACS on STN 



ACCESSION NUMBER: 
DOCUMENT NUMBER: 
TITLE: 

INVENTOR (S) : 



PATENT ASSIGNEE (S) : 
SOURCE : 

DOCUMENT TYPE: 
LANGUAGE : 

FAMILY ACC. NUM. COUNT: 
PATENT INFORMATION: 



2002 : 637634 HCAPLUS 
137:190735 

Novel succinate salt of 0-desmethylvenlaf axine 

Hadfield, Anthony Francis; Shah, Syed Muzafar; 

Winkley, Michael William; Sutherland, Karen Wiggins; 

Provost, James Andrew; Park, Aeri; Shipplett, Rex 

Alwyn; Russell, Brenton William; Weber, Beat Theodor 

Wyeth, John, and Brother Ltd., USA 

PCT Int. Appl., 76 pp. 

CODEN: PIXXD2 

Patent 

English 

1 



PATENT NO. 



KIND 



DATE 



WO 2002064543 

WO 2002064543 
W: AE, AG, 
CO, CR, 
GM, HR, 
LS, LT, 
PL, PT, 
UA, UG, 
RW: GH, GM, 
CY, DE, 
BF, BJ, 

CA 2436668 

US 2003045583 

US 6673838 

EP 1360169 

R: AT, BE, 
IE, SI, 

BR 2002007157 



AL, 
CU, 
HU, 
LU, 
RO, 
UZ, 
KE, 
DK, 
CF, 



CH, 
LT, 



CN 


1501909 


JP 


2004529877 


NO 


2003003533 


US 


2004044241 


ZA 


2003007116 


US 


2005096479 



A2 

A3 
AM, 
CZ, 
ID, 
LV, 
RU, 
VN, 
LS, 
ES, 
CG, 

AA 

Al 

B2 

A2 
DE, 
LV, 

A 

A 

T2 

A 

Al 

A 

Al 



20020822 
20021212 
AT, AU, AZ, 
DE, DK, DM, 
IL, IN, IS, 
MA, MD, MG, 
SD, SE, SG, 
YU, ZA, ZM, 
MW, MZ, SD, 
FI, FR, GB, 
CI, CM, GA, 
20020822 
20030306 
20040106 
20031112 
DK, ES, FR, 
FI, RO, MK, 
20040217 
20040602 
20040930 
20030811 
20040304 
20041213 
20050505 



APPLICATION NO. 



WO 2002-US4103 



DATE 



20020211 



BA, BB, BG, 

DZ, EC, EE, 

JP, KE, KG, 

MK, MN, MW, 

SI, SK, SL, 

ZW, AM, AZ, 

SL, SZ, TZ, 

GR, IE, IT, 

GN, GQ, GW, 
CA 2002- 



BR, BY, 

ES, FI, 

KP, KR, 

MX, MZ, 

TJ, TM, 

BY, KG, 

UG, ZM, 

LU, MC, 

ML, MR, 
2436668 



PRIORITY APPLN. INFO. 



US 


2002- 


73743 


EP 


2002- 


718949 


GR, IT, 


LI, LU 


AL, TR 




BR 


2002- 


7157 


CN 


2002- 


808112 


JP 


2002- 


564477 


NO 


2003- 


3538 


US 


2003- 


654756 


ZA 


2003- 


7116 


US 


2004- 


985292 


US 


2001- 


268214P 


US 


2001- 


297963P 


US 


2002- 


73743 



BZ, CA, CH, CN, 
GB, GD, GE, GH, ' 
KZ, LC, LK, LR, 
NO, NZ, OM, PH, 
TN, TR, TT, TZ, 
KZ, MD, RU, TJ, TM 
ZW, AT, BE, CH, 
NL, PT, SE, TR, 
NE, SN, TD, TG 
20020211 
20020211 

20020211 
NL, SE, MC, PT, 



20020211 
20020211 
20020211 
20030811 
20030904 
20030911 
20041110 
20010212 
20010613 



P 
P 

A3 20020211 



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Page 32 of 51 



wo 2002-US4103 W 20020211 

US 2003-654756 B3 20030904 

GI 



He 
• li— He 




AB A novel salt of 0-desmethyl venlafaxine (I) is provided, I succinate. 

Pharmaceutical compns . , dosage forms and methods of use are also provided. 
Examples are given for the prepn. of I, I monosuccinate and its 
monohydrate. 
93413-62-8 / O-Desmethyl venlafaxine 

RL: PRP (Properties); RCT (Reactant) ; THU (Therapeutic use) ; 
BIOL (Biological study); RACT (Reactant or reagent); USES (Uses) 
(0-desmethylvenlafaxine succinate crystal forms) 
RN 93413-62-8 HCAPLUS 

CN Phenol, 4- [2- (dimethyl amino) -1- ( 1-hydroxycyclohexyl) ethyl] - ( 9CI) (CA 
INDEX NAME) 




IT 386750-22-7 P 448904-47-O P 

RL: PRP (Properties); SPN (Synthetic preparation); THU (Therapeutic 
use); BIOL (Biological study); PREP (Preparation); USES (Uses) 
(0-desmethylvenlafaxine succinate crystal forms) 
RN 386750-22-7 HCAPLUS 

CN Butanedioic acid, compd. with 4- [2- (dimethylamino) -1- (l- 
hydroxycyclohexyl) ethyl] phenol (1:1), monohydrate (9CI) (CA INDEX NAME) 

CM 1 

CRN 93413-62-8 
CMF C16 H25 N 02 




CM 2 

CRN 110-15-6 
CMF C4 H6 04 



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RN 448904-47-0 HCAPLUS 

CN Butanedioic acid, compd. with 4- [2- (diitiethylamino) -1- (l- 
hydroxycyclohexyl) ethyl] phenol (1:1) OCX) (CA INDEX NAME) 

CM 1 

CRN 93413-62-8 
CMF C16 H25 N 02 




CM 2 

CRN 110-15-6 
CMF C4 H6 04 



IT 448904-48-i 

RL: RCT (Reactant) ; THU (Therapeutic use) ; BIOL (Biological 
study); RACT (Reactant or reagent); USES (Uses) 

(0-desmethylvenlafaxine succinate crystal forms) 
RN 448904-48-1 HCAPLUS 

CN Butanedioic acid, compd. with 4- [2- (dimethylamino) -1- (1- 

hydroxycyclohexyl) ethyl] phenol (1:2) (9CI) (CA INDEX NAME) 

CM 1 

CRN 93413-62-8 
CMF C16 H25 N 02 























i 
















T 

















CM 2 

CRN 110-15-6 
CMF C4 H6 04 



L4 ANSWER 24 OF 38 HCAPLUS COPYRIGHT 2005 ACS on STN 



ACCESSION NUMBER: 
DOCUMENT NUMBER: 
TITLE: 



2002 : 310162 HCAPLUS 

136:395834 

Combining bupropion SR with venlafaxine, paroxetine, 
or fluoxetine: A preliminary report on 



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Page 34 of 51 



pharmacokinetic, therapeutic, and sexual dysfunction 
effects 

AUTHOR(S): Kennedy, Sidney H.; McCann, Sonia M.; Masellis, Mario; 

Mclntyre, Roger S.; Raskin, Joel; McKay, Gordon; 
Baker, Glen B. 

CORPORATE SOURCE: Centre for Addiction and Mental Health, and the 

Department of Psychiatry, University of Toronto, 
Toronto, ON, Can. 

SOURCE: Journal of Clinical Psychiatry (2002), 63(3), 181-186 

CODEN: JCLPDE; ISSN: 0160-6689 
PUBLISHER: Physicians Postgraduate Press, Inc. 

DOCUMENT TYPE: Journal 
LANGUAGE: English 

AB This study was designed to evaluate the effect of combining bupropion 
sustained release (SR) with venlafaxine, paroxetine, or fluoxetine in 
patients who reported unacceptable sexual dysfunction when treated with 
monotherapy with the latter 3 agents. Following a min. of 6 wk of 
antidepressant treatment with a selective serotonin reuptake inhibitor 
(SSRI) or venlafaxine (a serotonin-norepinephrine reuptake inhibitor), 
eligible subjects received a further 8 wk of monitored combination therapy 
with bupropion SR at a dose of 150 mg/day with no alterations to index 
antidepressant dosing. There was a clin. significant benefit in 14 (78%) 
of 18 partial responders or nonresponders , and 33% (N = 6) achieved a full 
response (x2 = 8.06, df = 2, p =.017). Sexual dysfunction, 
particularly a decrease in orgasmic delay, was also significantly improved 
with combination therapy (men: paired t = -2.1, df = 6, p =.08; women: 
paired t = -3.0, df = 7, p =.02) . Plasma monitoring of drugs and their 
metabolites revealed a statistically significant increase in venlafaxine 
levels (F = 6.89, df = 4,24; p =.001) accompanied by a decrease in 
0-desmethyl-venlafaxine (F = 14.26; df = 4,24; p <.0005) during combined 
treatment with bupropion SR. There were no statistically significant 
changes in plasma levels of SSRIs (paroxetine and fluoxetine) during the 
trial. Bupropion had an effect on the pharmacokinetics of venlafaxine but 
not those of the SSRIs. Further investigation of combination treatments 
under randomized, double-blind conditions is recommended. 

IT 93413-62-8 / 0-Desmethylvenlaf axine 

RL: ADV (Adverse effect, including toxicity); PAC (Pharmacological 
activity); PKT (Pharmacokinetics); THU (Therapeutic use) ; BIOL 
(Biological study) ; USES (Uses) 

(bupropion SR with venlafaxine, paroxetine, or fluoxetine in sexual 
dysfunction patients with previous monotherapy treatment) 

RN 93413-62-8 HCAPLUS 

CN Phenol, 4- [2- (dimethylamino) -1- ( 1-hydroxycyclohexyl) ethyl] - (9CI) (CA 
INDEX NAME) 



HO 



Me 2N-CH2 




OH. 



REFERENCE COUNT: 



37 THERE ARE 37 CITED REFERENCES AVAILABLE FOR THIS 
RECORD. ALL CITATIONS AVAIIABLE IN THE RE FORMAT 



L4 ANSWER 25 OF 38 HCAPLUS COPYRIGHT 2005 ACS on STN 



ACCESSION NUMBER: 
DOCUMENT NUMBER: 



2002 : 248775 HCAPLUS 
136:318772 



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TITLE: False-positive phencyclidine immunoassay results 

caused by venlafaxine and 0-desmethylvenlafaxine 
Sena, Salvador F.; Kazimi, Syed; Wu, Alan H. B. 
Department of Pathology and Laboratory Medicine/ 
Danbury Hospital, Danbury, CT, 06810, USA 
Clinical Chemistry (Washington, DC, United States) 
(2002), 48(4), 676-677 
CODEN: CLCHAU; ISSN: 0009-9147 
American Association for Clinical Chemistry 
Journal 
English 

The authors believe that the data strongly implicate venlafaxine and 
0-desmethylvenlafaxine as the agents responsible for the false-pos. 
phencyclidine results the authors obsd. with the RapidTest device. 
IT 93413-62-8 / O-Desmethylvenlaf axine 

RL: ARU (Analytical role, unclassified); THU (Therapeutic use); 
ANST (Analytical study); BIOL (Biological study); USES (Uses) 

(phencyclidine false-pos. immunoassay results caused by venlafaxine and 
0-desmethylvenlafaxine) 
93413-62-8 HCAPLUS 

(9CI) (CA 



AUTHOR (S) : 
CORPORATE SOURCE: 

SOURCE : 



PUBLISHER: 
DOCUMENT TYPE: 
LANGUAGE : 
AB 



RN 
CN 



Phenol, 4- [2- (dimethylamino) ~1- ( 1-hydroxycyclohexyl) ethyl] 
INDEX NAME) 



Me2N-CH2 



HO 



CH — 



OH. 



REFERENCE COUNT: 



THERE ARE 7 CITED REFERENCES AVAILABLE FOR THIS 
RECORD. ALL CITATIONS AVAILABLE IN THE RE FORMAT 



ANSWER 




ACCESSION NUMBER: 
DOCUMENT NUMBER: 
TITLE: 

INVENTOR (S) : 
PATENT ASSIGNEE (S) 
SOURCE : 



DOCUMENT TYPE: 
LANGUAGE : 

FAMILY ACC. NUM. COUNT: 
PATENT INFORMATION: 



HCAPLUS COPYRIGHT 2005 ACS on STN 



2002 : 143294 HCAPLUS 
136: 189323 

Preparation and pharmaceutical formulation of 

enantiomers of 0-desmethyl venlafaxine 

Yardley, John P.; Asselin, Andre A. 

American Home Products Corporation, USA 

U.S. Pat. Appl. Publ., 8 pp., Cont. of U.S. Ser. No. 

590, 741, abandoned. 

CODEN: USXXCO 

Patent 

English 

2 



PATENT NO. 


KIND 


DATE 


APPLICATION NO. 




DATE 


US 2002022662 


Al 


20020221 


US 


2001-957908 




20010921 


US 2002161055 


Al 


20021031 


US 


2002-154994 




20020523 


US 2003149112 


Al 


20030807 


US 


2003-373145 




20030224 


US 2004176468 


Al 


20040909 


US 


2004-799321 




20040312 


US 2005256206 


Al 


20051117 


US 


2005-183573 




20050718 


PRIORITY APPLN. INFO. : 






US 


1999-183029P 


P 


19990615 








US 


2000-590741 


Bl 


20000608 








us 


2001-957908 


Al 


20010921 








US 


2002-154994 


Bl 


20020523 



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us 2003-373145 Al 20030224 

US 2004-799321 Bl 20040312 

AB This invention provides pharmaceutically active enantiomers of the 

venlafaxine metabolite 0-Desmethyl venlafaxine, R (-) -4- [2- (Dimethyl amnino) - 
1- ( 1-hydroxycyclo-hexyl) ethyl]phenol or R (-) 1- [2- (dimethyl ami no) -1- (4- 
hydroxyphenyl) ethyl] cyclo-hexanol (I) , and S ( + ) -1- [2- (Dimethylamino) -1- (4- 
hydroxyphenyl) ethyl] cyclohexanol or S (+) -4- [2- (Dimethylamino) -1- (1- 
hydroxycyclohexyl) ethyl] phenol, or one or more pharmaceutically acceptable 
salts or salt hydrates thereof, as well as pharmaceutical compns . 
utilizing these enantiomers and methods of using the enantiomers to treat, 
inhibit or control central nervous system disorders. To a soln. of 
1- [2- (Dimethylamino) -1- ( 4-methoxyphenyl ) ethyl] -cyclohexanol free base 
(prepn. given) in EtOAc at room temp, was added at once to a soln. of 
(+)-Di-para toluoyl-D-tartaric acid-monohydrate {DT(-)T) and was stirred 
at room temp, for 1 h. The resulting ppt. was filtered off, washed with 
EtOAc , dried overnight at 35? in a vacuum oven to provide crude 
R (-) -1- [2- (dimethylamino) -1- (4-methoxyphenyl) -ethyl] cyclohexanol DT (-) T 
salt (yield = 92.8%) as a white solid. The solid was recrystd., and 
treated with sodium hydroxide soln. to obtain I base which was sepd. and 
purified. Neurotransmitter uptake inhibition activity of the enantiomers 
were studied in rats. Pharmaceutical formulations of different 
enantiomers are disclosed. 

IT 93413-62-8P 

RL: PAC (Pharmacological activity); RCT (Reactant) ; SPN (Synthetic 
preparation); THU (Therapeutic use) ; BIOL (Biological study); 
PREP (Preparation); RACT (Reactant or reagent); USES (Uses) 

(prepn. and pharmaceutical formulation of enantiomers of desmethyl 
venlafaxine) 
RN 93413-62-8 HCAPLUS 

CN Phenol, 4-[2- (dimethylamino) -1- (1-hydroxycyclohexyl) ethyl] - (9CI) (CA 
INDEX NAME) 




L4 ANSWER 27 OF 38 HCAPLUS COPYRIGHT 2005 ACS on STN 



ACCESSION NUMBER: 
DOCUMENT NUMBER: 
TITLE : 



AUTHOR (S) : 



CORPORATE SOURCE: 



2002 : 111809 HCAPLUS 
136:288525 

Distribution of venlafaxine and its O-desmethyl 
metabolite in human milk and their effects in 
breastfed infants 

Ilett, Kenneth F.; Kristensen, Judith H.; Hac]<ett, 
Peter; Paech, Michael; Kohan, Rolland; Rampono, 
Jonathan 

Department of Pharmacology, University of Western 
Australia, Nedlands, 6009, Australia 
British Journal of Clinical Pharmacology (2002), 
53(1), 17-22 

CODEN: BCPHBM; ISSN: 0306-5251 
Blackwell Science Ltd. 
Journal 
English 

AB Aims: To characterize milk/plasma (M/P) ratio and infant dose, for 

venlafaxine (V) and its O-desmethyl metabolite (ODV) , in breastfeeding 



SOURCE : 



PUBLISHER: 
DOCUMENT TYPE: 
LANGUAGE : 



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Page 37 of 51 



women taking venlafaxine for the treatment of depression, and to det. the 
plasma concn. and effects of these drugs in their infants. Methods: Six 
women (mean age 34.5 yr, mean wt. 84.3 kg) taking venlafaxine (median dose 
244 mg day-1, range 225-300 mg day-1) and their seven infants (mean age 
7.0 mo, mean wt . 7.3 kg) were studied. V and ODV in plasma and milk were 
measured by high-performance liq. chromatog. over a 12 h dose interval at 
steady-state. Infant exposure was estd. as the product of estd. milk 
prodn. rate (0.15 1 kg-1 day-1) and av. drug concn. in milk, normalized to 
body wt. and expressed as a percentage of the wt. -adjusted maternal dose. 
Results: Mean M/PAUC values of 2.5 (range 2.0-3.2) and 2.7 (range 2.3-3.2) 
were calcd. for V and ODV, resp. The mean max. concns. (95% CI) of V and 
ODV in milk were 1161 (95% CI, 588, 1734) |ig 1-1 and 796 (362, 1230) 
\xg 1-1. Mean infant exposure was 3.2% (1.7, 4.7%) for V and 3.2% (1.9, 
4.9%) for ODV (as V equiv. ) . V was detected in the plasma of one out of 
seven infants studied (5 jig 1-1), while ODV was detected in four of the 
infants, at concns. ranging from 3 to 38 \ig 1-1. All of the infants in 
the study were healthy, as reported by their mothers and/or by clin. 
examn. on the study day. Conclusions: The concns. of V and ODV in breast 
milk were 2.5 and 2.7 times those in maternal plasma. The mean total drug 
exposure (as venlafaxine equiv.) of the breastfed infants was 6.4% 
(5.5-7.3%), which is below the 10% notional level of concern. There were 
no adverse effects in any of the infants. The data support the use of V 
in breastfeeding. Nevertheless, since low concns. of ODV were detected in 
the plasma of four out of the seven infants studied, we recommend 
breastfed infants should be monitored closely. Each decision to breast 
feed should be made as an individual risk: benefit anal. 

IT 93413-62-8 , 0-Desmethylvenlaf axine 

RL: ADV (Adverse effect, including toxicity); PAC (Pharmacological 
activity); PKT (Pharmacokinetics); THU (Therapeutic use); BIOL 
(Biological study); USES (Uses) 

(venlafaxine (Efexor) and metabolite 0-desmethylvenlaf axine 
distribution in human milk and effect in breastfed infants) 

RN 93413-62-8 HCAPLUS 

CN Phenol, 4- [2- (dimethylamino) -1- ( 1-hydroxycyclohexyl ) ethyl] - (9CI) (CA 
INDEX NAME) 



HO 



• Me2N-CH2 



(M 



REFERENCE COUNT: 



31 THERE ARE 31 CITED REFERENCES AVAILABLE FOR THIS 
RECORD. ALL CITATIONS AVAILABLE IN THE RE FORMAT 



L4 



ANSWER 2 8 OF 38 HCAPLUS COPYRIGHT 2005 ACS on STN 



ACCESSION NUMBER: 
DOCUMENT NUMBER: 
TITLE : 

AUTHOR (S) : 
CORPORATE SOURCE: 

SOURCE : 



PUBLISHER: 



2001 : 8797 60 HCAPLUS 
136:145144 

Effect of antidepressants on ATP-dependent calciiom 
uptake by neuronal endoplasmic reticulum 
Couture, L.; Elie, R.; Lavoie, P. -A. 

Departement de pharmacologie, Universite de Montreal, 
Montreal, QC, H3C 3J7, Can. 

Canadian Journal of Physiology and Pharmacology 
(2001), 79(11), 946-952 
CODEN: CJPPA3; ISSN: 0008-4212 
National Research Council of Canada 



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Page 38 of 51 



DOCUMENT TYPE: Journal 
LANGUAGE: English 

AB This study investigated the effect of tricyclic and atypical 

antidepressants on ATP dependent calcium uptake by the endoplasmic 
reticulum of lysed synaptosomes from rat brain cortex. Tricyclic 
antidepressants (imipramine, desipramine, clomipramine, amitriptyline) 
exhibited no effect in the lower range (0.06 to 2 |jM) of drug concns . , 
and a concn . -dependent inhibition of calcium uptake in the upper range (6 
to 200 pM) , A concn. -dependent inhibition was obsd. for atypical 
antidepressants (mianserin, desmethylmianserin, venlafaxine, 
desmethylvenlafaxine, fluoxetine) in both the lower and the upper range of 
drug concns. Since no stimulation of calcium uptake was obsd. in either 
concn, range, it appears that the tricyclic and atypical antidepressants 
tested are not capable of normalizing, through their effect on the 
endoplasmic reticulum, an overactive calcium signal, which is possibly 
implicated in the etiol. of affective disorders. Also, although only 
marginal inhibition of calcium uptake is expected at brain concns. of 
tricyclics and mianserin-desmethylmianserin that are likely to be 
encountered during clin. use, a more substantial inhibition could occur 
with fluoxetine. 

IT 93413-62"8 ^ 0-Desmethyl venlafaxine 

RL: PAC (Pharmacological activity); THU (Therapeutic use); BIOL 
(Biological study); USES (Uses) 

(effect of antidepressants on ATP-dependent calcium uptake by neuronal 
endoplasmic reticulum) 

RN 93413-62-8 HCAPLUS 

CN Phenol, 4- [2- (dimethylamino) -1- ( 1-hydroxycyclohexyl) ethyl] - (9CI) (CA 
INDEX NAME) 



Me 2N-CH2 

CHr 



HO 




OH 



REFERENCE COUNT: 



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RECORD. ALL CITATIONS AVAILABLE IN THE RE FORMAT 



L4 ANSWER 29 OF 38 HCAPLUS COPYRIGHT 2005 ACS on STN 



Ful 


1 rxtiii^ 


Tex 





ACCESSION NUMBER: 
DOCUMENT NUMBER: 
TITLE: 

INVENTOR (S) : 
PATENT ASSIGNEE (S) : 
SOURCE : 

DOCUMENT TYPE: 
L7\NGUAGE : 

FAMILY ACC. NUM. COUNT: 
PATENT INFORMATION: 



2000: 900601 HCAPLUS 
134:56475 

Preparation and formulation of O-desmethyl venlafaxine 
enantiomers 

Yardley, John Patrick; Asselin, Andre Alfred 

American Home Products Corporation, USA 

PCT Int. Appl., 24 pp. 

CODEN: PIXXD2 

Patent 

English 

2 



PATENT NO. KIND DATE 



WO 2000076955 Al 20001221 

W: AE, AG, AL, AM, AT, AU, AZ, 
CU, CZ, DE, DK, DM, DZ, EE, 



APPLICATION NO. DATE 



WO 2000-US16388 20000614 
BA, BB, BG, BR, BY, CA, CH, CN, CR, 
ES, FI, GB, GD, GE, GH, GM, HR, HU, 



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11/22/05 



Page 39 of 51 



ID, 


IL, 


IN, 


IS, 


JP, 


KE, 


KG, 


KP, 


KR, 


KZ, 


LC, 


LK, 


LR, 


LS, 


LT, 


LU, 


LV, 


MA, 


MD, 


MG, 


MK, 


MN, 


MW, 


MX, 


MZ, 


NO, 


NZ, 


PL, 


PT, 


RO, 


RU, 


SD, 


SE, 


SG, 


SI, 


SK, 


SL, 


TJ, 


TM, 


TR, 


TT, 


TZ, 


UA, 


UG, 


UZ, 


VN, 


YU, 


ZA, ZW 


GH, 


GM, 


KE, 


LS, 


MW, 


MZ, 


SD, 


SL, 


SZ, 


TZ, 


UG, 


ZW, 


AT, 


BE, 


CH, 


CY, 


DE, 


DK, 


ES, 


FI, 


FR, 


GB, 


GR, 


IE, 


IT, 


LU, 


MC, 


NL, 


PT, 


SE, 


BF, 


BJ, 




CG, 


CI, 


CM, 


GA, 


GN, 


GW, 


ML, 


MR, 


NE, 


SN, 


TD, 


TG 









PRIORITY APPLN. INFO.: US 1999-183029P P 19990615 

US 1999-333594 A 19990615 

AS Title compds. were prepd. by optical resoln. of venlafaxine followed by 

O-demethylation. Data for biol. activity of title compds. were given. 
IT 142761-11-3P 142761-12-4 P 313471-76-OP , 

(R) -(-) -O-Desmethyl venlafaxine fumarate hydrate 313474-92-'9 P, 

(S) -(+) -O-Desmethyl venlafaxine fumarate hydrate 

RL: BAG (Biological activity or effector, except adverse); BSU (Biological 
study, unclassified) ; SPN (Synthetic preparation) ; THU (Therapeutic 
use); BIOL (Biological study); PREP (Preparation); USES (Uses) 

(prepn. and formulation of 0-desmethyl venlafaxine enantiomers) 
RN 142761-11-3 HCAPLUS 

CN Phenol, 4-t {lR)-2- (dimethylamino) -1- ( 1-hydroxycyclohexyl) ethyl] - (9CI) 
(CA INDEX NAME) 

Absolute stereochemistry. Rotation (-) . 



^NHe2 




RN 142761-12-4 HCAPLUS 

CN Phenol, 4- [ (IS) -2- (dimethylamino) -1- ( 1-hydroxycyclohexyl ) ethyl] - (9CI) 
(CA INDEX NAME) 

Absolute stereochemistry. Rotation (-i-) . 




RN 313471-76-0 HCAPLUS 

CN Phenol, 4- [ (IR) -2- (dimethylamino) -1- (1-hydroxycyclohexyl) ethyl] 

(2E)-2-butenedioate (1:1) (salt), monohydrate (9CI) (CA INDEX NAME) 

CM 1 

CRN 142761-11-3 
CMF C16 H25 N 02 

Absolute stereochemistry. Rotation (-) . 



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Page 40 of 51 




CM 2 

CRN 110-17-8 
CMF C4 H4 04 



Double bond geometry as shown. 

RN 313474-92-9 HCAPLUS 

CN Phenol, 4- [ (IS) -2- (dimethyl amino) -1- (1-hydroxycyclohexyl) ethyl] 

(2E)-2-butenedioate (1:1) (salt), monohydrate (9CI) (CA INDEX NAME) 

CM 1 

CRN 142761-12-4 
CMF C16 H25 N 02 

Absolute stereochemistry. Rotation (+) . 




CM 2 

CRN 110-17-8 
CMF C4 H4 04 



Double bond geometry as shown. 



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RECORD. ALL CITATIONS AVAILABLE IN THE RE FORMAT 



ANSWER 30 OF 38 HCAPLUS COPYRIGHT 2005 ACS on STN 



HCAPLUS 




ACCESSION NUMBER: 
DOCUMENT NUMBER: 
TITLE : 

INVENTOR (S) : 
PATENT ASSIGNEE (S) 
SOURCE : 



2000:725583 
133:296268 

Preparation of derivatives of venlafaxine and their 
inhibition of neuronal monoamine reuptake 
Jerussi^ Thomas P.; Senanayake, Chrisantha H. 
Sepracor Inc., USA 
PCT Int. Appl., 40 pp. 
CODEN: PIXXD2 



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11/22/05 



Page41of 51 



DOCUMENT TYPE: Patent 

LANGUAGE: English 

FAMILY ACC. NUM. COUNT: 1 
PATENT INFORMATION: 



PATENT NO. 



KIND DATE 



APPLICATION NO. 



DATE 



WO 


2000059851 




Al 




20001012 




WO 2000- 


US8705 




20000331 




W: AE, 


AG, 


AL, 


AM, 


AT, 


AU, 


AZ, 


BA, 


BB, BG, 


BR, 


BY, 


CA, 


CH, CN, CR, 




CU, 


CZ, 


DE, 


DK, 


DM, 


DZ, 


EE, 


ES, 


FI, GB, 


GD, 


GE, 


GH, 


GM, HR, HU, 




ID, 


IL, 


IN, 


IS, 


JP/ 


KE, 


KG, 


KP, 


KR, KZ, 


LC, 


LK, 


LR, 


LS, LT, LU, 




LV, 


MA, 


MD, 


MG, 


MK, 


MN, 


MW, 


MX, 


NO, NZ, 


PL, 


PT, 


RO, 


RU, SD, SE, 




SG, 


SI, 


SK, 


SL, 


TJ, 


TM, 


TR, 


TT, 


TZ, UA, 


UG, 


UZ, 


VN, 


YU, ZA, ZW, 




AM, 


AZ, 


BY, 


KG, 


KZ, 


MD, 


RU, 


TJ, 


TM 












RW: GH, 


GM, 


KE, 


LS, 


MW, 


SD, 


SL, 


SZ, 


TZ, UG, 


ZW, 


AT, 


BE, 


CH, CY, DE, 




DK, 


ES, 


FI, 


FR, 


GB, 


GR, 


IE, 


IT, 


LU, MC, 


NL, 


PT, 


SE, 


BF, BJ, CF, 




CG, 


CI, 


CM, 


GA, 


GN, 


GW, 


ML, 


MR, 


NE, SN, 


TD, 


TG 






CA 


2368083 






AA 




20001012 




CA 2000- 


2368083 




20000331 


EP 


1165487 






Al 




20020102 




EP 2000- 


920026 




20000331 




R: AT, 


BE, 


CH, 


DE, 


DK, 


ES, 


FR, 


GB, 


GR, IT, 


LI, 


LU, 


NL, 


SE, MC, PT, 




IE, 


SI, 


LT, 


LV, 


FI, 


RO 
















JP 


2003521470 




T2 




20030715 




JP 2000- 


609367 




20000331 


NZ 


514612 






A 




20040130 




NZ 2000- 


514612 




20000331 


EP 


1466889 






Al 




20041013 




EP 2004- 


10248 




20000331 




R: AT, 


BE, 


CH, 


DE, 


DK, 


ES, 


FR, 


GB, 


GR, IT, 


LI, 


LU, 


NL, 


SE, MC, PT, 




IE, 


SI, 


LT, 


LV, 


FI, 


RO, 


MK, 


CY, 


AL 










AU 


782092 






B2 




20050630 




AU 2000- 


40627 




20000331 


NO 


2001004816 




A 




20011204 




NO 2001- 


4816 






20011003 


US 


2004106576 




Al 




20040603 




US 2003- 


720134 




20031125 


US 


2005197392 




Al 




20050908 




US 2005- 


91518 




20050329 



PRIORITY APPLN. INFO. 



US 1999-127938P 
US 1999-167906P 
US 2000-527442 
EP 2000-920026 
WO 2000-US8705 
US 2003-720134 



P 19990406 
P 19991130 
A3 20000317 
A3 20000331 
W 20000331 
A3 20031125 



AB 



Prepn. of derivs. of venlafaxine, e.g., 0-desmethylvenlaf laxine, is 
described. Also disclosed are methods of treating and preventing diseases 
and disorders including, but not limited to, affective disorders such as 
depression, bipolar and manic disorders, attention deficit disorder, 
attention deficit disorder with hyperactivity, Parkinson's disease, 
epilepsy, cerebral function disorders, obesity and wt. gain, incontinence, 
dementia and related disorders. 
IT 300827-87-6 P 

RL: BAC (Biological activity or effector, except adverse); BSU (Biological 
study, unclassified) ; SPN (Synthetic preparation) ; THU (Therapeutic 
use); BIOL (Biological study); PREP (Preparation); USES (Uses) 

(prepn. of derivs. of venlafaxine and their inhibition of neuronal 
monoamine reuptake) 
300827-87-6 HCAPLUS 

Phenol, 4- [2- (dimethyl amino) -1- ( 1-hydroxycyclohexyl) ethyl] -, hydrochloride 
(9CI) (CA INDEX NAME) 



RN 
CN 



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Page 42 of 51 



Me 2N-CH2 



HO 



I'-O 



OH 



« HCl 

REFERENCE COUNT: 



THERE ARE 5 CITED REFERENCES AVAILABLE FOR THIS 
RECORD. ALL CITATIONS AVAILABLE IN THE RE FORMAT 



ANSWER 31 OF 38 HCAPLUS COPYRIGHT 2005 ACS on STN 



HCAPLUS 




ACCESSION NUMBER: 
DOCUMENT NUMBER: 
TITLE: 



AUTHOR (S) 



CORPORATE SOURCE: 



SOURCE : 



PUBLISHER: 

DOCUMENT TYPE: 
LANGUAGE : 
AB 



2000:700645 

134:163 

CYP2B6 mediates the in vitro hydroxylation of 
bupropion: potential drug interactions with other 
antidepressants 

Hesse, Leah M.; Venkatakrishnan, Karthik; Court, 
Michael H.; Von Moltke, Lisa L. ; Duan, Su X.; Shader, 
Richard I.; Greenblatt, David J. 
Department of Pharmacology and Experimental 

Therapeutics, New England Medical Center, Tufts 
University School of Medicine, Boston, MA, 02111, USA 
Drug Metabolism and Disposition (2000), 28(10), 
1176-1183 

CODEN: DMDSAI; ISSN: 0090-9556 

American Society for Pharmacology and Experimental 
Therapeutics 
Journal 
English 

The in vitro biotransformation of bupropion to hydroxybupropion was 
studied in human liver microsomes and microsomes contg. heterologously 
expressed human cytochromes P 450 (CYP) . The mean (?S.E.) Km in four 
human liver microsomes was 89 (?14) |iM. In microsomes contg. 
cDNA-expressed CYPs, hydroxybupropion formation was mediated only by 
CYP2B6 at 50 |iM bupropion (Km 85 |iM) . A CYP2B6 inhibitory antibody 
produced more than 95% inhibition of bupropion hydroxylation in four human 
livers. Bupropion hydroxylation activity at 250 ^iM was highly 
correlated with S-mephenytoin N-demethylation activity (yielding 
nirvanol) , another CYP2B6-mediated reaction, in a panel of 32 human livers 
(r = 0.94). The CYP2B6 content of 12 human livers highly correlated with 
bupropion hydroxylation activity (r = 0.96). Thus bupropion hydroxylation 
is mediated almost exclusively by CYP2B6 and can serve as an index 
reaction reflecting activity of this isoform. IC50 values for inhibition 
of a CYP2D6 index reaction (dextromethorphan 0-demethylation) by bupropion 
and hydroxybupropion were 58 and 74 ^M, resp. This suggests a low 
inhibitory potency vs. CYP2D6, the clin. importance of which is not 
established. Since bupropion is frequently coadministered with other 
antidepressants, IC50 values (pM) for inhibition of bupropion 
hydroxylation were detd. as follows: paroxetine (1.6), fluvoxamine (6.1), 
sertraline (3.2), desmethylsertraline (19.9), fluoxetine (59.5), 
norfluoxetine (4.2), and nefazodone (25.4). Bupropion hydroxylation was 
only weakly inhibited by venlafaxine, 0-desmethylvenlaf axine, citalopram, 
and desmethylcitalopram. The inhibition of bupropion hydroxylation in 
vitro by a no. of newer antidepressants suggests the potential for clin. 
drug interactions. 



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11/22/05 



Page 43 of 51 



IT 93413-62-8 , 0-Desmethylvenlaf axine 

RL: BAG (Biological activity or effector, except adverse); BSU (Biological 
study, unclassified) ; THU (Therapeutic use) ; BIOL (Biological 
study); USES (Uses) 

(CYP2B6 mediates in vitro hydroxylation of bupropion: potential drug 
interactions with other antidepressants) 
RN 93413-62-8 HCAPLUS 

ON Phenol, 4- [2- (dimethylamino) -1- (1-hydroxycyclohexyl) ethyl] - (9CI) (CA 
INDEX NAME) 



Me'2N-CH2 



HO 



XX' 




OH 



REFERENCE COUNT: 



41 THERE ARE 41 CITED REFERENCES AVAILABLE FOR THIS 
RECORD. ALL CITATIONS AVAILABLE IN THE RE FORMAT 



L4 



ANSWER 32 OF 38 HCAPLUS COPYRIGHT 2005 ACS on STN 



ACCESSION NUMBER: 
DOCUMENT NUMBER: 
TITLE : 

INVENTOR (S) : 
PATENT ASSIGNEE (S) : 
SOURCE : 

DOCUMENT TYPE: 
LANGUAGE : 

FAMILY ACC. NUM. COUNT: 
PATENT INFORMATION: 



2000: 384124 HCAPLUS 
133:17270 

Preparation of (-) -venlaf axine and derivatives as 

neuronal monoamine reuptake inhibitors. 

Jerussi, Thomas P.; Senanayake, Chrisantha H. 

Sepracor Inc., USA 

PCT Int. Appl., 45 pp. 

CODEN: PIXXD2 

Patent 

English 

1 



PATENT NO. KIND DATE APPLICATION NO. DATE 



WO 


2000032556 




Al 




20000608 




WO 1999- 


US28303 




19991201 




W: AE, 


AL, 


AM, 


AT, 


AU, 


AZ, 


BA, 


BB, 


BG, BR, 


BY, 


CA, 


CH, 


CN, CR, CU, 




CZ, 


DE, 


DK, 


EE, 


ES, 


FI, 


GB, 


GD, 


GE, GH, 


GM, 


HR, 


HU, 


ID, IL, IN, 




IS, 


JP, 


KE, 


KG, 


KP, 


KR, 


KZ, 


LC, 


LK, LR, 


LS, 


liT, 


LU, 


LV, MA, MD, 




MG, 


MK, 


MN, 


MW, 


MX, 


NO, 


NZ, 


PL, 


PT, RO, 


RU, 


SD, 


SE, 


SG, SI, SK, 




SL, 


TJ, 


TM, 


TR, 


TT, 


UA, 


UG, 


UZ, 


VN, YU, 


ZA, 


ZW, 


AM, 


AZ, BY, KG, 




KZ, 


MD, 


RU, 


TJ, 


TM 




















RW: GH, 


GM, 


KE, 


LS, 


MW, 


SD, 


SL, 


SZ, 


TZ, UG, 


ZW, 


AT, 


BE, 


CH, CY, DE, 




DK, 


ES, 


FI, 


FR, 


GB, 


GR, 


IE, 


IT, 


LU, MC, 


NL, 


PT, 


SE, 


BF, BJ, CF, 




CG, 


CI, 


CM, 


GA, 


GN, 


GW, 


ML, 


MR, 


NE, SN, 


TD, 


TG 






us 


6342533 






Bl 




20020129 




US 1999- 


450690 




19991130 


CA 


2352324 






AA 




20000608 




CA 1999- 


2352324 




19991201 


EP 


1135359 






Al 




20010926 




EP 1999- 


968056 




19991201 




R: AT, 


BE, 


CH, 


DE, 


DK, 


ES, 


FR, 


GB, 


GR, IT, 


LI, 


LU, 


NL, 


SE, MC, PT, 




IE, 


SI, 


LT, 


LV, 


FI, 


RO 
















JP 


2003524613 




T2 




20030819 




JP 2000- 


585198 




19991201 


AU 


774408 






B2 




20040624 




AU 2000- 


24749 




19991201 


US 


2002086904 




Al 




20020704 




US 2001- 


14592 




20011214 


US 


6441048 






B2 




20020827 














US 


2003018083 




Al 




20030123 




US 2002- 


222815 




20020819 


US 


6911479 






B2 




20050628 














US 


2004180952 




Al 




20040916 




US 2004- 


806423 




20040323 


PRIORITY APPLN. 


INFO 














US 1998- 


110488P 




P 19981201 



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11/22/05 



Page 44 of 51 



US 


1999- 


450690 


A 


19991130 


wo 


1999- 


US28303 


W 


19991201 


us 


2001- 


14592 


A3 


20011214 


us 


2002- 


222815 


A3 


20020819 



AB A pharmaceutical compn. comprising (-) -venlafaxine deriv. substantially 
free of {+) -stereoisomer is claimed. Thus, (?) -venlafaxine in THF was 
added to a mixt. prepd. from Ph2PH and BuLi in THF at 0? followed 
by stirring and overnight reflux to give 73.8% (?)-0- 

desmethyl venlafaxine, which was resolved using di-p-toluoyl-L-tartaric 
acid to give (-) -0-desmethylvenlafaxine . Drug formulations contg. the 
latter are given. 
IT 142761-12-4 P 

RL: BAG (Biological activity or effector, except adverse); BSU (Biological 
study, unclassified); PUR (Purification or recovery); SPN (Synthetic 
preparation); THU (Therapeutic use) ; BIOL (Biological study); 
PREP (Preparation); USES (Uses) 

(prepn. of {-) -venlafaxine and derivs. as neuronal monoamine reuptake 
inhibitors) 
RN 142761-12-4 HCAPLUS 

CN Phenol, 4- [ (IS) -2- (dimethylamino) -1- (1-hydroxycyclohexyl) ethyl] - (9CI) 
(CA INDEX NAME) 



Absolute stereochemistry. Rotation {+) . 




REFERENCE COUNT: 



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RECORD. ALL CITATIONS AVAILABLE IN THE RE FORMAT 



L4 ANSWER 33 OF 38 



HCAPLUS COPYRIGHT 2005 ACS on STN 



ACCESSION NUMBER: 
DOCUMENT NUMBER: 
TITLE: 

INVENTOR (S) : 
PATENT ASSIGNEE (S) : 
SOURCE : 

DOCUMENT TYPE: 
LANGUAGE : 

FAMILY ACC. NUM. COUNT: 
PATENT INFORMATION: 



2000: 384122 HCAPLUS 
133:30575 

Preparation of derivatives of (+) -venlafaxine as 

inhibitors of neuronal monoamine reuptake. 

Jerussi, Thomas P.; Senannayake, Chrisantha H. 

Sepracor Inc., USA 

PCT Int. Appl., 47 pp. 

CODEN : PIXXD2 

Patent 

English 

1 



PATENT NO. KIND DATE APPLICATION NO. DATE 

WO 2000032555 Al 20000608 WO 1999-US28306 19991201 

W: AE, AL, AM, AT, AU, AZ, BA, BB, BG, BR, BY, CA, CH, CN, CR, CU, 

CZ, DE, DK, EE, ES, FI, GB, GD, GE, GH, GM, HR, HU, ID, IL, IN, 

IS, JP, KE, KG, KP, KR, KZ, LC, LK, LR, LS, LT, LU, LV, MA, MD, 

MG, MK, MN, m, MX, NO, NZ, PL, PT, RO, RU, SD, SE, SG, SI, SK, 

SL, TJ, TM, TR, TT, UA, UG, UZ, VN, YU, ZA, ZW, AM, AZ, BY, KG, 

KZ, MD, RU, TJ, TM 

RW: GH, GM, KE, LS, MW, SD, SL, SZ, TZ, UG, ZW, AT, BE, CH, CY, DE, 



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DK, 


ES, 


FI, 


FR, 


GB, 


GR, IE, 


IT, 


LU, MC, 


NL, PT, 


SE, 


BF, BJ, CF, 




CG, 


CI, 


CM, 


GA, 


GN, 


GW, ML, 


MR, 


NE, SN, 


TD, TG 






US 


6197828 






Bl 




20010306 




US 1999- 


450691 




19991130 


CA 


2352321 






AA 




20000608 




CA 1999- 


2352321 




19991201 


EP 


1135358 






Al 




20010926 




EP 1999- 


965065 




19991201 




R: AT, 


BE, 


CH, 


DE, 


DK, 


ES, FR, 


GB, 


GR, IT, 


LI, LU, 


NL, 


SE, MC, PT, 




IE, 


FI 




















JP 


2003501344 




T2 




20030114 




JP 2000- 


585197 




19991201 


PRIORITY 


APPLN. 


INFO. 












US 1998- 


110486P 




P 19981201 


















US 1999- 


450691 




A 19991130 


















WO 1999- 


US28306 




W 19991201 



RN 
CN 



AB A method of treating an affective disorder comprises administration of a 
(+) -venlafaxine deriv. substantially free of the (-) -enantiomer . Thus, 
(?) -venlafaxine (prepn. given) was added to a 0? mixt. of Ph2PH 
and BuLi followed by stirring and reflux overnight to give 73.8% 
(?) -0-desmethylvenlafaxine, which was resolved to give 
(+) -O-desmethylvenlafaxine. Drug formulations contg. the latter are 
given. 

IT 142761-12-4P 

RL: BAG (Biological activity or effector, except adverse) ; BSU (Biological 
study, unclassified); PUR (Purification or recovery); SPN (Synthetic 
preparation) ; THU (Therapeutic use) ; BIOL (Biological study) ; 
PREP (Preparation); USES (Uses) 

(prepn. of derivs. of (+) -venlafaxine as inhibitors of neuronal 
monoamine reuptake) 
142761-12-4 HCAPLUS 



Phenol, 4- [ (IS) -2- (dimethyl amino) -1- ( 1-hydroxycyclohexyl) ethyl] - (9CI) 
(CA INDEX NAME) 



Absolute stereochemistry. Rotation (+) 



NMe2 




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ANSWER 34 OF 38 




ACCESSION NUMBER: 
DOCUMENT NUMBER: 
TITLE: 



INVENTOR (S) : 
PATENT ASSIGNEE (S) : 
SOURCE : 

DOCUMENT TYPE: 
LANGUAGE : 

FAMILY ACC. NUM. COUNT: 
PATENT INFORMATION: 



HCAPLUS COPYRIGHT 2005 ACS on STN 



1998 : 534794 HCAPLUS 
129:156948 

Modifying the behavior of dogs exhibiting canine 

affective aggression with R and S enantiomers or 

racemic mixtures of selective serotonin reuptake 

inhibitors or their metabolites 

Dodman, Nicholas H. 

Trustees of Tufts College, USA 

U.S., 21 pp., Cont . -in-part of U.S. 5,554,383. 

CODEN: USXXAM 

Patent 

English 

3 



PATENT NO. 



KIND DATE 



APPLICATION NO. 



DATE 



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US 5788986 


A 


19980804 


US 


1996-699112 


19960816 


US 5554383 


A 


19960910 


US 


1995-417747 


19950406 


PRIORITY APPLN. INFO. : 






US 


1995-417747 


A2 19950406 



AB A veterinary method for clin. modifying the behavior of a household pet 
dog exhibiting a recognized type of canine affective aggression behavior 
is provided. The veterinary behavior modification method administers at 
least one compd. selected from the group consisting of R enantiomers, S 
enantiomers, or a racemic mixt. of selective serotonin reuptake inhibitors 
or their active metabolites to the dog upon one or multiple occasions; and 
the administration of these compds. will modify clin. the canine affective 
aggression behavior of the household dog permanently or for an indefinite 
period of time. This veterinary behavior modification method can be 
usefully employed as an adjunct to conditioning approaches presently 
employed and will avoid the need for euthanasia in extreme behavioral 
circumstances. 

IT 93413-62-8 

RL: BAG (Biological activity or effector, except adverse); BSU (Biological 
study, unclassified) ; THU (Therapeutic use) ; BIOL (Biological 
study); USES (Uses) 

(modifying the behavior of aggressive dogs with R and S enantiomers or 
racemic mixts. of selective serotonin reuptake inhibitors or their 
metabolites) 
RN 93413-62-8 HCAPLUS 

CN Phenol, 4- [2- (dimethyl amino) -1- (1-hydroxycyclohexyl) ethyl] - (9CI) (CA 
INDEX NAME) 



:;ho 



Me 2N-CH2 




OH:; 



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L4 



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HCAPLUS 







^■1 


Text 







ACCESSION NUMBER: 
DOCUMENT NUMBER: 
TITLE: 



1997:681434 
127:355027 

Application of a first-pass effect model to 
characterize the pharmacokinetic disposition of 
venlafaxine after oral adjninistration to human 
subjects 

Taft, David R.; Iyer, Ganesh R.; Behar, Leon; 
DiGregorio, Robert V. 

Division of Pharmaceutics and Industrial Pharmacy, 
Long Island University, Brooklyn, NY, 11201, USA 
Drug Metabolism and Disposition (1997), 25(10), 
1215-1218 

CODEN: DMDSAI; ISSN: 0090-9556 
Williams & Wilkins 
Journal 
English 

Venlafaxine (VEN) , a drug used in the treatment of depression, undergoes 
significant first-pass metab. after oral dosing to 0-desmethyl venlafaxine 
(ODV) , a metabolite with comparable therapeutic activity to that of parent 
drug. The pharmacokinetic disposition of VEN was characterized using a 
"first-pass" model that incorporates a presystemic compartment (liver) to 



AUTHOR (S) 



CORPORATE SOURCE: 



SOURCE : 



PUBLISHER: 
DOCUMENT TYPE: 
LANGUAGE : 
AB 



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account for the first-pass metab. of VEN to ODV. A series of differential 
equations were simultaneously fitted to plasma concns. of parent and 
metabolite. A good fit of the model to obsd. data was demonstrated, 
generating ests. for the following parameters: ka (1.31 h-1) , WEN (252 
L), CLint (65.8 L/h) , RL (liver : plasma partition coeff., 29.6), VODV (181 
L), and CLODV (23.5 L/h) . Parameter ests. correlated closely with those 
obtained through noncompartmental methods. These results indicate that 
the time-course disposition of a compd. undergoing first-pass hepatic 
metab. after oral dosing can be successfully modeled. 
IT 93413-62-8 . 0-Desmethylvenlaf axine 

RL: BPR (Biological process); BSU (Biological study, unclassified); MFM 
(Metabolic formation) ; THU (Therapeutic use) ; BIOL (Biological 
study); FOKK (Formation, nonpreparative) ; PROC (Process); USES (Uses) 
(application of a first-pass effect model to characterize the 
pharmacokinetic disposition of venlafaxine after oral administration to 
human subjects) 
93413-62-8 HCAPLUS 

CN Phenol, 4- [2- (dimethyl ami no) -1- ( 1-hydroxycyclohexyl) ethyl] - (9CI) (CA 
INDEX NAME) 



Me 2N-CH2 



HO 



XT 



"in 

CH ^ 



dH 



REFERENCE COUNT: 



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RECORD. ALL CITATIONS AVAILABLE IN THE RE FORMAT 



L4 



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HCAPLUS 



ACCESSION NUMBER 
DOCUMENT NUMBER: 
TITLE: 



AUTHOR (S) 
CORPORATE 

SOURCE : 



SOURCE : 



Frazer, 
Med. , 



Alan 



(1997), 6(1), 



1997:43252 
126: 139312 

Central & peripheral nervous systems. Venlafaxine: a 
novel antidepressant compound 
Schweizer, Edward; Thielen, Richard J.; 
Dep. Psychiary, Univ. Pennsylvania Sch. 
Philadelphia, PA, 19104, USA 
Expert Opinion on Investigational Drugs 
65-78 

CODEN: EOIDER; ISSN: 0967-8298 
Ashley Publications 
Journal; General Review 
English 

A review, with 89 refs. Venlafaxine is a new antidepressant that inhibits 
the reuptake of both 5-hydroxytryptamine (serotonin; 5-HT) and 
noradrenaline (NA) . It is somewhat more potent as an inhibitor of the 
reuptake of 5-HT than NA. Its potency to inhibit the reuptake of 5-HT is 
comparable to that of tricyclic antidepressants (TCAs) such as 
amitriptyline or imipramine, but it is less potent than these drugs at 
inhibiting the reuptake of NA. Consequently, at low doses, venlafaxine 
may be a more effective inhibitor of the reuptake of 5-HT than that of NA. 
The major metabolite of venlafaxine in humans, 0-desmethylvenlaf axine, has 
comparable potency to the parent drug for inhibiting the reuptake of 
either NA or 5-HT in vitro, but it is less potent in vivo. Both 
venlafaxine and 0-desmethyl venlafaxine are essentially devoid of activity 
at muscarinic cholinergic, HI histaminergic, and |3l-adrenoceptors . 
This probably account for venlafaxine having a side-effect profile similar 



PUBLISHER: 
DOCUMENT TYPE 
LANGUAGE : 
AB 



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to that of selective serotonin reuptake inhibitors (SSRIs) rather than 
that of TCAs. Venlafaxine is subject to extensive first-pass metab. and 
is metabolized by the cytochrome P 450 isoenzyme IID6 in the liver. The 
half-life of venlafaxine is 3-4 h and that of its principal metabolite is 
about 10 h. The daily dose of venlafaxine can be administered as either 
two or three divided doses without altering significantly the 
pharmacokinetics of venlafaxine. The most common side-effects of 
venlafaxine are nausea, sedation, and dizziness, dry mouth and sweating, 
as well as sexual dysfunctions, primarily problems with erection and 
delayed ejaculation. In some patients, venlafaxine also caused sustained 
elevations in both systolic and diastolic blood pressure; this effect is 
dose-dependent. Venlafaxine is much safer in over-dosage than the TCAs. 
Antidepressant efficacy of venlafaxine has been found in out-patients and 
in-patients. In general, its efficacy is comparable to that of comparator 
drugs (primarily TCAs or SSRIs), and in some cases even greater, and its 
efficacy is greater than that measured with placebo. 
IT 93413-62-8 ^ 0-Desmethylvenlaf axine 

RL: BAC (Biological activity or effector, except adverse); BSU (Biological 
study, unclassified); MFM (Metabolic formation); THU (Therapeutic 
use); BIOL (Biological study); FORM (Formation, nonpreparative) ; USES 
(Uses) 

(venlafaxine antidepressant activity and pharmacokinetics in humans) 
RN 93413-62-8 HCAPLUS 

CN Phenol, 4- [2- (dimethylamino) -1- (1-hydroxycyclohexyl) ethyl] - (9CI) (CA 
INDEX NAME) 



:;H0: 



Me2H-CH2 




GH 



REFERENCE COUNT: 



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ANSWER 37 OF 38 

1^ 




HCAPLUS COPYRIGHT 2005 ACS on STN 



ACCESSION NUMBER: 
DOCUMENT NUMBER: 
TITLE : 

INVENTOR (S) : 
PATENT ASSIGNEE (S) : 
SOURCE : 

DOCUMENT TYPE: 
LANGUAGE : 

FAMILY ACC. NUM. COUNT: 
PATENT INFORMATION: 



1991:81228 HCAPLUS 
114:81228 

Preparation of cyclohexanol derivatives as 

intermediates for antidepressants 

Shepherd, Robin Gerald 

John Wyeth and Brother Ltd., UK 

Brit. UK Pat. Appl . , 15 pp. 

CODEN : BAXXDU 

Patent 

English 

1 



PATENT NO. 



GB 2227743 

GB 2227743 

US 5043466 
PRIORITY APPLN. INFO. 
OTHER SOURCE (S) : 
GI 



KIND 

Al 
B2 
A 



DATE 



19900808 
19920617 
19910827 



APPLICATION NO. 

GB 1990-2095 

US 1990-471187 
GB 1989-2209 



CASREACT 114:81228; MARPAT 114:81228 



DATE 

19900130 

19900126 
A 19890201 



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t\\2-me2 III 

AB Title compds. I [Rl = cyano, C0NMe2, CSNMe2; R2 = OMe, (protected) OH], 
useful as intermediates for prepn. of antidepressants, were prepd. by 
reaction of II [M = Li, Na, K, or MgX (X = halo); R2 = OMe, protected OH] 
witli cyclohexanone in hydrocarbon/ether solvents. For example, II (Rl = 
CSNMe2, R2 = OMe, M = MgBr) gave the corresponding I in 64% yield. 
Subsequent redn. of I by Raney~Ni gave the antidepressant (no data) 
N,N-dimethyl-2- (1-hydroxycyclohexyl) -2- (4-methoxyphenyl) ethylamine (III) . 

IT 93413-62-8 P 

RL: BAG (Biological activity or effector, except adverse); BSU (Biological 
study, unclassified) ; SPN (Synthetic preparation) ; THU (Therapeutic 
use); BIOL (Biological study); PREP (Preparation); USES (Uses) 
(prepn. of, as antidepressant) 
RN 93413-62-8 HCAPLUS 

CN Phenol, 4- [2- (dimethyl ami no) -1- (1-hydroxycyclohexyl) ethyl] - (9CI) (CA 
INDEX NAME) 



::H0: 




-CH.2 




OH: 



L4 ANSWER 38 OF 38 HCAPLUS COPYRIGHT 2005 ACS on STN 



ACCESSION NUMBER: 
DOCUMENT NUMBER: 
TITLE : 

AUTHOR (S) : 



CORPORATE SOURCE: 
SOURCE : 



DOCUMENT TYPE: 
LANGUAGE : 
OTHER SOURCE (S) : 
GI 



1990: 630878 HCAPLUS 
113:230878 

2-Phenyl-2- ( 1-hydroxycycloalkyl ) ethylamine 
derivatives: synthesis and antidepressant activity 
Yardley, John P.; Husbands, G. E. Morris; Stack, Gary; 
Butch, Jacqueline; Bicksler, James; Moyer, John A. ; 
Muth, Eric A.; Andree, Terrance; Fletcher, Horace, 
III; et al. 

Wyeth-Ayerst Res., Princeton, NJ, 08543-8000, USA 
Journal of Medicinal Chemistry (1990), 33(10), 
2899-905 

CODEN: JMCMAR; ISSN: 0022-2623 

Journal 

English 

CASREACT 113:230878 



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4 




AB A series of 2-phenyl-l- (1-hydroxycycloalkyl) ethylamine derivs. was examd. 

for the ability to inhibit both rat brain imipramine receptor binding and 
the synaptosomal uptake of norepinephrine (NE) and serotonin (S-HT) . 
Neurotransmitter uptake inhibition was highest for a subset of 
2-phenyl-2- (1-hydroxycyclohexyl) dimethylethylamines in which the aryl ring 
has a halogen or methoxy substituent at the 3- and/or 4-positions. 
Potential antidepressant activity in this subset was assayed in three 
rodent models-the antagonism of reserpine-induced hypothermia, the 
antagonism of histamine-induced ACTH release, and the ability to reduce 
noradrenergic responsiveness in the rat pineal gland. An acute effect 
seen in the rat pineal gland with several analogs, including 
1- [1- (3, 4-dichlorophenyl) -2- (dimethyl amino) ethyl] cyclohexanol and 
1- [2- (dimethylamino) -1- (4-methoxyphenyl) ethyl] cyclohexanol (I) , was taken 
as a possible correlate of a rapid onset of antidepressant activity. 
Compd. I (venlafaxine) is presently undergoing clin. evaluation. 

IT 93413-62-8 P 93414-04-lP 

RL: BAG (Biological activity or effector, except adverse) ; BSU (Biological 
study, unclassified) ; SPN (Synthetic preparation) ; THU (Therapeutic 
use); BIOL (Biological study); PREP (Preparation); USES (Uses) 
(prepn. and antidepressant activity of) 

RN 93413-62-8 HCAPLUS 

CN Phenol, 4- [2- (dimethylamino) -1- ( 1-hydroxycyclohexyl ) ethyl] - (9CI) (CA 
INDEX NAME) 




RN 93414-04-1 HCAPLUS 

CN Phenol, 4- [2- (dimethylamino) -1- ( 1-hydroxycyclohexyl ) ethyl] -, 
(2E)-2-butenedioate (1:1) (salt) (9CI) (CA INDEX NAME) 



CM 1 



CRN 93413-62-8 
CMF C16 H25 N 02 




CM 2 

CRN 110-17-8 
CMF C4 H4 04 

Double bond geometry as shown. 



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=> 



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